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Cat.Nr.S7397
| Gerelateerde doelwitten | ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Overige Raf Inhibitoren | LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) PLX-4720 AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265) |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| MV-4-11 | Growth Inhibition Assay | IC50=0.00000303 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.00418 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=0.03184 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=0.07416 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.25022 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=0.47073 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.5636 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=0.65613 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.85088 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=0.88818 μM | SANGER | |||
| GDM-1 | Growth Inhibition Assay | IC50=0.90698 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=1.02098 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=1.20809 μM | SANGER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=1.21678 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=1.35578 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=1.37648 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=1.47935 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=1.59165 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=1.61726 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=1.63812 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=1.8098 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=1.8842 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=2.1448 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.21393 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.3162 μM | SANGER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=2.39764 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=2.42242 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=2.69609 μM | SANGER | |||
| K052 | Growth Inhibition Assay | IC50=2.74616 μM | SANGER | |||
| L-540 | Growth Inhibition Assay | IC50=2.75789 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=2.8135 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=2.92185 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=3.06299 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=3.12003 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=3.13162 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=3.47509 μM | SANGER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=3.61468 μM | SANGER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=3.66099 μM | SANGER | |||
| BC-1 | Growth Inhibition Assay | IC50=3.7402 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=3.83673 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=3.88198 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=4.16815 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=4.23391 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=4.28798 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=4.40484 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=4.48905 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=5.07294 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=5.13227 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=5.24929 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=5.41685 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=5.50824 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=5.73568 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=5.95682 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=6.00678 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=6.25266 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=6.31839 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=6.45866 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=6.52849 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=6.61062 μM | SANGER | |||
| SIMA | Growth Inhibition Assay | IC50=7.00101 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=7.05676 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=7.05989 μM | SANGER | |||
| NB1 | Growth Inhibition Assay | IC50=7.40407 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=7.62663 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=7.76503 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=7.84511 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=8.40002 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=8.63133 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=8.63746 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=8.76353 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=9.10834 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=9.11243 μM | SANGER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=9.21026 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=9.71662 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=9.7561 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=9.76029 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=10.4745 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=10.5441 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=10.7526 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=11.1216 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=11.3876 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=11.9044 μM | SANGER | |||
| CHP-126 | Growth Inhibition Assay | IC50=11.9738 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=12.0278 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=12.0985 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=12.5413 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=12.5479 μM | SANGER | |||
| NCI-H1522 | Growth Inhibition Assay | IC50=12.746 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=13.2911 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=13.5126 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=13.6046 μM | SANGER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=13.8555 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=14.0609 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=14.1551 μM | SANGER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=14.4811 μM | SANGER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=14.9616 μM | SANGER | |||
| ECC4 | Growth Inhibition Assay | IC50=15.0558 μM | SANGER | |||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=15.4131 μM | SANGER | |||
| SCH | Growth Inhibition Assay | IC50=15.4728 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=15.6534 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=16.0714 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=16.1297 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=16.1661 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=16.189 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=16.6119 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=17.006 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=17.0072 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=17.1638 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=17.6833 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=17.8344 μM | SANGER | |||
| COR-L279 | Growth Inhibition Assay | IC50=18.1362 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=18.7143 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=18.8041 μM | SANGER | |||
| LU-165 | Growth Inhibition Assay | IC50=19.7008 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=20.3184 μM | SANGER | |||
| RL | Growth Inhibition Assay | IC50=20.9692 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=21.1889 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=21.3752 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=21.3946 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=21.3992 μM | SANGER | |||
| PF-382 | Growth Inhibition Assay | IC50=21.4403 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=21.5615 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=21.6394 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=21.8513 μM | SANGER | |||
| Daudi | Growth Inhibition Assay | IC50=21.9304 μM | SANGER | |||
| D-542MG | Growth Inhibition Assay | IC50=22.0256 μM | SANGER | |||
| U-698-M | Growth Inhibition Assay | IC50=22.4603 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=22.7366 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=23.8897 μM | SANGER | |||
| ECC12 | Growth Inhibition Assay | IC50=24.2803 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=24.3239 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=24.4362 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=24.5221 μM | SANGER | |||
| DMS-153 | Growth Inhibition Assay | IC50=24.8614 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=25.0265 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=26.3414 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=26.5796 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=26.8535 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=26.9828 μM | SANGER | |||
| THP-1 | Growth Inhibition Assay | IC50=27.2141 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=27.332 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=27.6231 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=29.1746 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=30.7278 μM | SANGER | |||
| NCI-H2227 | Growth Inhibition Assay | IC50=30.9806 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=31.4492 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=32.0826 μM | SANGER | |||
| EVSA-T | Growth Inhibition Assay | IC50=32.2585 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=33.1101 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=33.1603 μM | SANGER | |||
| NCI-H2196 | Growth Inhibition Assay | IC50=33.2557 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=33.3135 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=33.8638 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=33.9956 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=34.2296 μM | SANGER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=34.9451 μM | SANGER | |||
| NCI-H1963 | Growth Inhibition Assay | IC50=35.3072 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=35.8785 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=36.0654 μM | SANGER | |||
| WSU-NHL | Growth Inhibition Assay | IC50=36.164 μM | SANGER | |||
| CESS | Growth Inhibition Assay | IC50=36.2848 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=36.5835 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=37.1237 μM | SANGER | |||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=37.1821 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=38.43 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=39.0733 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=39.8432 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=40.3096 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=41.5805 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=42.8406 μM | SANGER | |||
| DG-75 | Growth Inhibition Assay | IC50=43.7595 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=45.4058 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=45.5758 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=46.1873 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=46.434 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=46.4756 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=47.1405 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=49.0791 μM | SANGER | |||
| NCI-H748 | Growth Inhibition Assay | IC50=49.4753 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=49.6628 μM | SANGER | |||
| MV4-11 | Antiproliferative activity assay | IC50 = 0.00087 μM | 19754199 | |||
| MV4-11 | Cytotoxicity assay | IC50 = 0.00087 μM | 19654408 | |||
| TT | Antiproliferative activity assay | IC50 = 0.0014 μM | 18849971 | |||
| RS4-11 | Function assay | IC50 = 0.002 μM | 19654408 | |||
| MOLM13 | Function assay | IC50 = 0.002 μM | 24641103 | |||
| Sf9 | Function assay | IC50 = 0.003 μM | 21708468 | |||
| RS4-11 | Function assay | IC50 = 0.0032 μM | 19654408 | |||
| MV4-11 | Growth inhibition assay | IC50 = 0.004 μM | 29357250 | |||
| A375 | Function assay | IC50 = 0.0044 μM | 29461827 | |||
| MOLM13 | Antiproliferative activity assay | IC50 = 0.005 μM | 24641103 | |||
| MV4-11 | Function assay | IC50 = 0.007 μM | 23362959 | |||
| MV4-11 | Cytotoxicity assay | IC50 = 0.007 μM | 26342867 | |||
| HEK293 | Function assay | Kd = 0.013 μM | 19754199 | |||
| Kasumi-1 | Antiproliferative activity assay | IC50 = 0.015 μM | 20570526 | |||
| MV4-11 | Antiproliferative activity assay | IC50 = 0.015 μM | 20570526 | |||
| sf9 | Function assay | IC50 = 0.015 μM | 29266937 | |||
| sf9 | Function assay | IC50 = 0.018 μM | 21708468 | |||
| sf9 | Function assay | IC50 = 0.02 μM | 23618709 | |||
| MV4-11 | Antiproliferative activity assay | GI50 = 0.03 μM | 21708468 | |||
| Sf9 | Function assay | IC50 = 0.042 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.043 μM | 18473434 | |||
| MV4-11 | Cytotoxicity assay | GI50 = 0.043 μM | 23618709 | |||
| MV4-11 | Function assay | GI50 = 0.043 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.044 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.054 μM | 21708468 | |||
| SF9 | Function assay | IC50 = 0.054 μM | 23618709 | |||
| MOLM13 | Antiproliferative activity assay | GI50 = 0.056 μM | 21708468 | |||
| MOLM13 | Antiproliferative activity assay | GI50 = 0.056 μM | 22726931 | |||
| MOLM13 | Cytotoxicity assay | GI50 = 0.056 μM | 23618709 | |||
| MOLM-13 | Function assay | GI50 = 0.056 μM | 26081023 | |||
| SF9 | Function assay | IC50 = 0.058 μM | 29266937 | |||
| WM266.4 | Antiproliferative activity assay | IC50 = 0.06 μM | 25496804 | |||
| MDA-MB-231 | Function assay | IC50 = 0.063 μM | 28431342 | |||
| SF9 | Function assay | IC50 = 0.09 μM | 29266937 | |||
| Spodoptera frugiperda | Function assay | IC50 = 0.09 μM | 26922228 | |||
| SF9 | Function assay | IC50 = 0.09 μM | 23562241 | |||
| SF9 | Function assay | IC50 = 0.1 μM | 23442188 | |||
| SF9 | Function assay | IC50 = 0.1 μM | 23442188 | |||
| HEK293 | Function assay | IC50 = 0.12 μM | 26318998 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 0.19 μM | 25496804 | |||
| MV4-11 | Antiproliferative activity human | IC50 = 0.3 μM | 28242553 | |||
| HepG2 | Antiproliferative activity assay | EC50 = 0.302 μM | 27010810 | |||
| THP1 | Antiproliferative activity assay | IC50 = 0.31 μM | 20570526 | |||
| SMMC7721 | Cytotoxicity assay | IC50 = 0.37 μM | 25982075 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 0.39 μM | 25778995 | |||
| sf9 | Function assay | Kd = 0.6 μM | 28109791 | |||
| T47D | Antiproliferative activity assay | IC50 = 0.61 μM | 25778995 | |||
| A549 | Cytotoxicity assay | IC50 = 0.63 μM | 25982075 | |||
| HeLa | Cytotoxicity assay | IC50 = 0.64 μM | 30015070 | |||
| WM3629 | Antiproliferative activity assay | GI50 = 0.65 μM | 20466542 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 0.65 μM | 26342134 | |||
| WM3629 | Growth inhibition assay | GI50 = 0.78 μM | 20149658 | |||
| WM3629 | Antiproliferative activity assay | GI50 = 0.78 μM | 26810260 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 0.78 μM | 25778995 | |||
| K562 | Antiproliferative activity assay | IC50 = 0.86 μM | 24315192 | |||
| COLO205 | Antiproliferative activity assay | IC50 = 0.87 μM | 25778995 | |||
| T29 | Cytotoxicity assay | IC50 = 0.9 μM | 26318998 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 0.94 μM | 25086238 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 0.94 μM | 25440879 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 1.06 μM | 29628325 | |||
| BL21(DE3) | Function assay | IC50 = 1.1 μM | 19928858 | |||
| K562 | Antiproliferative activity assay | IC50 = 1.22 μM | 25778995 | |||
| MDA-MB-231 | Growth inhibition assay | GI50 = 1.26 μM | 28088086 | |||
| MDA-MB-231 | Cytotoxicity assay | GI50 = 1.26 μM | 26590508 | |||
| MDA-MB-231 | Antiproliferative activity assay | GI50 = 1.26 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | EC50 = 1.3 μM | 18942827 | |||
| sf9 | Function assay | Kd = 1.3 μM | 28109791 | |||
| F-6-8 | Cytotoxicity assay | IC50 = 1.3 μM | 26318998 | |||
| A549 | Antiproliferative activity assay | IC50 = 1.45 μM | 26342134 | |||
| rhabdomyosarcoma | Antiviral activity assay | EC50 = 1.5 μM | 27288186 | |||
| HL-60(TB) | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| RPMI8226 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| KM12 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| LOXIMVI | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| HCT116 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| HOP92 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| SF539 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| UACC62 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| SF295 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| MDA-MB-435 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| SK-MEL-5 | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| T47D | Growth inhibition assay | GI50 = 1.58 μM | 28088086 | |||
| RPMI8266 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| HL-60(TB) | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| KM12 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| HCT116 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SF295 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SF539 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SK-MEL-2 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| MDA-MB-435 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SK-MEL-5 | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| LOXIMVI | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| T47D | Cytotoxicity assay | GI50 = 1.58 μM | 26590508 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 1.58 μM | 26753815 | |||
| LOXIMVI | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| UACC62 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| SK-MEL-5 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| KM12 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| MDA-MB-435 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| SF539 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| SF295 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| HCT116 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| HOP92 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| RPMI8226 | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| HL-60(TB) | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| T47D | Antiproliferative activity assay | GI50 = 1.58 μM | 27017549 | |||
| 7dF3 | Function assay | IC50 = 1.62 μM | 29266937 | |||
| MDA-MB-435 | Antiproliferative activity assay | IC50 = 1.67 μM | 25778995 | |||
| HL60 | Cytotoxicity assay | IC50 = 1.68 μM | 24858546 | |||
| SW579 | Antiproliferative activity human | IC50 = 1.73 μM | 28242553 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 1.88 μM | 25637123 | |||
| A375P | Antiproliferative activity assay | IC50 = 1.9 μM | 24128410 | |||
| A549 | Cytotoxicity assay | IC50 = 1.92 μM | 24826815 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 2 μM | 22808911 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 2 μM | 23454017 | |||
| NCI-H23 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| NCI-H522 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| HOP62 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| NCI-H226 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| HT-29 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| U251 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| COLO205 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| CCRF-CEM | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| MALME-3M | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| M14 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| UACC257 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| PC3 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| SK-MEL-2 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| MDA-MB-468 | Growth inhibition assay | GI50 = 2 μM | 28088086 | |||
| CCRF-CEM | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| NCI-H23 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| NCI-H522 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| COLO205 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| HT-29 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| SK-MEL-28 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| HOP62 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| UACC257 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| NCI-H226 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| U251 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| PC3 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| M14 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| MDA-MB-468 | Cytotoxicity assay | GI50 = 2 μM | 26590508 | |||
| PC3 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| MALME-3M | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| U251 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| UACC257 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| SK-MEL-2 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| COLO205 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| NCI-H23 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| M14 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| NCI-H226 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| HOP62 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| MDA-MB-468 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| CCRF-CEM | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| NCI-H522 | Antiproliferative activity assay | GI50 = 2 μM | 27017549 | |||
| A549 | Antiproliferative activity assay | IC50 = 2.02 μM | 26753815 | |||
| MDA-MB-435 | Growth inhibition assay | IC50 = 2.11 μM | 29189002 | |||
| NCI-H460 | Antiproliferative activity assay | IC50 = 2.19 μM | 30216849 | |||
| H460 | Cytotoxicity assay | IC50 = 2.19 μM | 24826815 | |||
| H460 | Cytotoxicity assay | IC50 = 2.19 μM | 25086238 | |||
| H460 | Cytotoxicity assay | IC50 = 2.19 μM | 25440879 | |||
| A375 | Toxicity assay | IC50 = 2.2 μM | 19654408 | |||
| H460 | Antiproliferative activity assay | IC50 = 2.25 μM | 26991938 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 2.3 μM | 23260578 | |||
| MKN45 | Antiproliferative activity assay | IC50 = 2.32 μM | 30216849 | |||
| MKN45 | Cytotoxicity assay | IC50 = 2.32 μM | 24826815 | |||
| MKN45 | Cytotoxicity assay | IC50 = 2.32 μM | 25086238 | |||
| MKN45 | Cytotoxicity assay | IC50 = 2.32 μM | 25440879 | |||
| U937 | Antiproliferative activity assay | GI50 = 2.34 μM | 29459144 | |||
| A375 | Antiproliferative activity assay | IC50 = 2.4 μM | 22808911 | |||
| HeLa | Growth inhibition assay | IC50 = 2.44 μM | 29102175 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 2.5 μM | 22414612 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 2.51 μM | 30216849 | |||
| UO31 | Antiproliferative activity assay | IC50 = 2.51 μM | 30216849 | |||
| NCI-H322M | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| NCI-H460 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| KM12 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| LOXIMVI | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| EKVX | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| HCT116 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| SW620 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SF268 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SF539 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| A498 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| UACC62 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| IGROV1 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| HCT15 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SK-MEL-28 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SK-MEL-28 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| ACHN | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SK-MEL-5 | Growth inhibition assay | TGI = 2.51 μM | 28088086 | |||
| NCI/ADR-RES | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| MCF7 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SN12C | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| Hs 578T | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| SKOV3 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| UO31 | Growth inhibition assay | GI50 = 2.51 μM | 28088086 | |||
| NCI-H460 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| HCT15 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SW620 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SF268 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| IGROV1 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| OVCAR8 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| NCI/ADR-RES | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SKOV3 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| SN12C | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| NCI-H322M | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| MCF7 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| UO31 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| Hs578T | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| A498 | Cytotoxicity assay | GI50 = 2.51 μM | 26590508 | |||
| A498 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SKOV3 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| UO31 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| NCI-ADR-RES | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SN12C | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| IGROV1 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| ACHN | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| OVCAR8 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| NCI-H322M | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SF268 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| HCT15 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| NCI-H460 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| SW620 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| EKVX | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| MCF7 | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| Hs 578T | Antiproliferative activity assay | GI50 = 2.51 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 2.58 μM | 29886324 | |||
| A375P | Antiproliferative activity assay | GI50 = 2.58 μM | 26810260 | |||
| TPC1 | Antiproliferative activity assay | EC50 = 2.6 μM | 22559926 | |||
| Hep3B | Growth inhibition assay | IC50 = 2.63 μM | 29102175 | |||
| A375P | Antiproliferative activity assay | IC50 = 2.7 μM | 22460030 | |||
| U937 | Antiproliferative activity assay | GI50 = 2.74 μM | 26318067 | |||
| U937 | Cytotoxicity assay | GI50 = 2.74 μM | 24878193 | |||
| MCF7 | Growth inhibition assay | IC50 = 2.78 μM | 29102175 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 2.8 μM | 29202403 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 2.84 μM | 28242553 | |||
| U937 | Growth inhibition assay | GI50 = 2.85 μM | 22014755 | |||
| A549 | Cytotoxicity assay | IC50 = 2.92 μM | 28927801 | |||
| A549 | Cytotoxicity assay | IC50 = 2.92 μM | 27777009 | |||
| ZR75-30 | Growth inhibition assay | IC50 = 2.96 μM | 29102175 | |||
| PC3 | Cytotoxicity assay | IC50 = 3.03 μM | 28340913 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 3.08 μM | 26991938 | |||
| A549 | Growth inhibition assay | IC50 = 3.1 μM | 29102175 | |||
| K562 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| MOLT4 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| A549/ATCC | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| RPMI8226 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| SR | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| HOP62 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| NCI-H226 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| U251 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| COLO205 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| M14 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| HCC2998 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| SNB75 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| 786-0 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| A498 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| HCT15 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| OVCAR3 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| OVCAR4 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| Caki1 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| SNB19 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| OVCAR5 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| DU145 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| OVCAR8 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| SN12C | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| MDA-MB-231 | Growth inhibition assay | TGI = 3.16 μM | 28088086 | |||
| RXF393 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| BT549 | Growth inhibition assay | GI50 = 3.16 μM | 28088086 | |||
| K562 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| MOLT4 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| SNB19 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| SR | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| A549 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| OVCAR3 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| OVCAR4 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| SNB75 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| OVCAR5 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| DU145 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| 786-0 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| BT549 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| ACHN | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| Caki1 | Cytotoxicity assay | GI50 = 3.16 μM | 26590508 | |||
| 786-0 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| LOXIMVI | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| Caki1 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| OVCAR5 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| RXF393 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SNB75 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| OVCAR3 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SNB19 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SK-MEL-5 | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| OVCAR4 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SK-MEL-2 | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| BT549 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| MOLT4 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| K562 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| HCC2998 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| HCC2998 | Antiproliferative activity assay | TGI = 3.16 μM | 27017549 | |||
| A549/ATCC | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| DU145 | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| SR | Antiproliferative activity assay | GI50 = 3.16 μM | 27017549 | |||
| MCF7 | Cytotoxicity assay | IC50 = 3.18 μM | 28927801 | |||
| PC3 | Cytotoxicity assay | IC50 = 3.18 μM | 28927801 | |||
| MCF7 | Cytotoxicity assay | IC50 = 3.18 μM | 27777009 | |||
| A549 | Antiproliferative activity assay | IC50 = 3.19 μM | 25778995 | |||
| PC3 | Cytotoxicity assay | IC50 = 3.24 μM | 27777009 | |||
| HeLa | Function assay | IC50 = 3.3 μM | 15225706 | |||
| HeLa | Function assay | IC50 = 3.3 μM | 15225706 | |||
| LoVo | Cytotoxicity assay | IC50 = 3.3 μM | 23454017 | |||
| A375 | Antiproliferative activity assay | IC50 = 3.36 μM | 29602674 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 3.37 μM | 26991938 | |||
| FLT3 gene-deficient U937 | Antiproliferative activity assay | GI50 = 3.4 μM | 21708468 | |||
| FLT3 negative U937 | Cytotoxicity assay | GI50 = 3.4 μM | 23618709 | |||
| U937 | Cytotoxicity assay | GI50 = 3.4 μM | 26081023 | |||
| A375P | Antiproliferative activity assay | GI50 = 3.4 μM | 29459144 | |||
| ACHN | Cytotoxicity assay | IC50 = 3.4 μM | 29517908 | |||
| ACHN | Cytotoxicity assay | IC50 = 3.4 μM | 29297688 | |||
| HepG2 | Function assay | IC50 = 3.4 μM | 26071861 | |||
| A375P | Cytotoxicity assay | GI50 = 3.4 μM | 24878193 | |||
| HepG2 | Cytotoxicity assay | IC50 = 3.44 μM | 28927801 | |||
| HepG2 | Cytotoxicity assay | IC50 = 3.44 μM | 27777009 | |||
| ACHN | Cytotoxicity assay | IC50 = 3.5 μM | 29786436 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 3.5 μM | 25462265 | |||
| HT-29 | Cytotoxicity assay | IC50 = 3.61 μM | 24826815 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 3.61 μM | 30216849 | |||
| HT-29 | Cytotoxicity assay | IC50 = 3.61 μM | 25086238 | |||
| HT-29 | Cytotoxicity assay | IC50 = 3.61 μM | 25440879 | |||
| MCF7 | Anticancer activity assay | IC50 = 3.64 μM | 29549841 | |||
| Sf9 | Function assay | IC50 = 3.8 μM | 21708468 | |||
| Sf9 | Function assay | IC50 = 3.8 μM | 23618709 | |||
| Sf9 | Function assay | IC50 = 3.8 μM | 26081023 | |||
| A2058 | Cytotoxicity assay | IC50 = 3.8 μM | 22708987 | |||
| NCI-H460 | Cytotoxicity assay | IC50 = 3.9 μM | 23454017 | |||
| SK-MEL-30 | Cytotoxicity assay | IC50 = 3.9 μM | 29461827 | |||
| HT-29 | Anticancer activity assay | IC50 = 3.97 μM | 29549841 | |||
| SF268 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| SNB75 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| OVCAR3 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| SNB19 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| Hs 578T | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| TK10 | Growth inhibition assay | GI50 = 3.98 μM | 28088086 | |||
| BT549 | Growth inhibition assay | TGI = 3.98 μM | 28088086 | |||
| Caki1 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| TK10 | Antiproliferative activity assay | GI50 = 3.98 μM | 27017549 | |||
| MDA-MB-435 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| HCT116 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| MDA-MB-231 | Antiproliferative activity assay | TGI = 3.98 μM | 27017549 | |||
| HepG2 | Cytotoxicity assay | IC50 = 4 μM | 23454017 | |||
| HT-29 | Cytotoxicity assay | IC50 = 4 μM | 23454017 | |||
| A549 | Cytotoxicity assay | IC50 = 4 μM | 23454017 | |||
| HuH7 | Cytotoxicity assay | GI50 = 4 μM | 23726028 | |||
| PC3 | Antiproliferative activity assay | IC50 = 4.13 μM | 25778995 | |||
| HeLa | Cytotoxicity assay | IC50 = 4.163 μM | 23362959 | |||
| MDA-MB-436 | Antiproliferative activity assay | IC50 = 4.2 μM | 29202403 | |||
| MCF7 | Cytotoxicity assay | IC50 = 4.21 μM | 27043268 | |||
| MCF7 | Cytotoxicity assay | IC50 = 4.21 μM | 28340913 | |||
| LOXIMVI | Antiproliferative activity assay | IC50 = 4.25 μM | 25778995 | |||
| OVCAR4 | Cytotoxicity assay | TGI = 4.31 μM | 26590508 | |||
| WM1361 | Antiproliferative activity assay | GI50 = 4.345 μM | 20148563 | |||
| WM266.4 | Growth inhibition assay | GI50 = 4.5 μM | 20199087 | |||
| HepG2 | Cytotoxicity assay | GI50 = 4.5 μM | 23726028 | |||
| A549 | Antiproliferative activity assay | IC50 = 4.5 μM | 23260578 | |||
| LS174T | Function assay | IC50 = 4.52 μM | 29266937 | |||
| 8505C | Antiproliferative activity assay | IC50 = 4.7 μM | 29032031 | |||
| OVCAR8 | Cytotoxicity assay | TGI = 4.73 μM | 26590508 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 4.77 μM | 20435479 | |||
| B16-F1 | Antiproliferative activity assay | IC50 = 4.9 μM | 18477505 | |||
| WM164 | Antiproliferative activity assay | IC50 = 4.9 μM | 17561392 | |||
| B16-F1 | Antiproliferative activity assay | IC50 = 4.9 μM | 20056548 | |||
| MDA-MB-468 | Cytotoxicity assay | IC50 = 4.9 μM | 26159483 | |||
| 786-O | Cytotoxicity assay | IC50 = 4.9 μM | 29517908 | |||
| 786-O | Cytotoxicity assay | IC50 = 4.9 μM | 29297688 | |||
| WM266.4 | Antiproliferative activity assay | GI50 = 4.933 μM | 20148563 | |||
| WM266.4 | Growth inhibition assay | IC50 = 5 μM | 19323560 | |||
| WM164 | Antiproliferative activity assay | IC50 = 5 μM | 20056548 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 5 μM | 23260578 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 5 μM | 23932071 | |||
| NCI-H23 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| NCI-H322M | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| NCI-H460 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| NCI-H522 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| HT-29 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| CCRF-CEM | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| SW620 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| HOP92 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| 786-0 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| MDA-MB-435 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| PC3 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| UACC257 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| SKOV3 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| RXF393 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| T47D | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| MDA-MB-468 | Growth inhibition assay | TGI = 5.01 μM | 28088086 | |||
| UACC62 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| UACC257 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| SK-MEL-5 | Antiproliferative activity assay | LC50 = 5.01 μM | 27017549 | |||
| M14 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| NCI-H23 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| SF295 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| HOP92 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| BT549 | Antiproliferative activity assay | TGI = 5.01 μM | 27017549 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 5.1 μM | 26159483 | |||
| DU145 | Cytotoxicity assay | IC50 = 5.1 μM | 22708987 | |||
| A549 | Cytotoxicity assay | IC50 = 5.21 μM | 20181414 | |||
| HeLa | Cytotoxicity assay | IC50 = 5.23 μM | 26342867 | |||
| 786-O | Cytotoxicity assay | IC50 = 5.3 μM | 29786436 | |||
| HCT116 | Antiproliferative activity assay | GI50 = 5.4 μM | 15225706 | |||
| A375 | Antiproliferative activity assay | IC50 = 5.4 μM | 18477505 | |||
| SK-MEL-188 | Antiproliferative activity assay | IC50 = 5.4 μM | 17561392 | |||
| A375 | Antiproliferative activity assay | IC50 = 5.4 μM | 20056548 | |||
| MCF7 | Cytotoxicity assay | IC50 = 5.5 μM | 26159483 | |||
| A375 | Antiproliferative activity assay | IC50 = 5.58 μM | 19464887 | |||
| A375P | Cytotoxicity assay | IC50 = 5.58 μM | 20797858 | |||
| A375P | Antiproliferative activity assay | GI50 = 5.58 μM | 21353571 | |||
| A375P | Growth inhibition assay | GI50 = 5.58 μM | 22014755 | |||
| A375P | Growth inhibition assay | GI50 = 5.58 μM | 20149658 | |||
| A375P | Antiproliferative activity assay | GI50 = 5.58 μM | 20466542 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 19857963 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 21592628 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 22033063 | |||
| A375P | Cytotoxicity assay | IC50 = 5.6 μM | 19897366 | |||
| A375P | Antiproliferative activity assay | IC50 = 5.6 μM | 22647720 | |||
| HCT116 | Cytotoxicity assay | IC50 = 5.65 μM | 24215818 | |||
| SH-SY5Y | Antiproliferative activity assay | IC50 = 5.73 μM | 24315192 | |||
| HepG2 | Cytotoxicity assay | IC50 = 5.74 μM | 25461318 | |||
| Bel7402 | Cytotoxicity assay | IC50 = 5.8 μM | 23454017 | |||
| HT-29 | Cytotoxicity assay | IC50 = 5.9 μM | 28865276 | |||
| melanoma | Growth inhibition assay | IC50 = 6.1 μM | 16392826 | |||
| K562 | Antiproliferative activity assay | GI50 = 6.2 μM | 21708468 | |||
| HepG2 | Cytotoxicity assay | IC50 = 6.2 μM | 28865276 | |||
| A549 | Anticancer activity assay | IC50 = 6.21 μM | 29549841 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 6.23 μM | 22721924 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 6.3 μM | 23932071 | |||
| SF295 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| SK-MEL-2 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| OVCAR5 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| UO31 | Growth inhibition assay | TGI = 6.31 μM | 28088086 | |||
| A498 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| MALME-3M | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| U251 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| SK-MEL-2 | Antiproliferative activity assay | LC50 = 6.31 μM | 27017549 | |||
| RPMI8226 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| HCC2998 | Antiproliferative activity assay | LC50 = 6.31 μM | 27017549 | |||
| NCI-H522 | Antiproliferative activity assay | TGI = 6.31 μM | 27017549 | |||
| HUVEC | Antiproliferative activity assay | IC50 = 6.42 μM | 23644219 | |||
| A549 | Cytotoxicity assay | IC50 = 6.53 μM | 27043268 | |||
| A549 | Cytotoxicity assay | IC50 = 6.53 μM | 28340913 | |||
| LoVo | Antiproliferative activity assay | IC50 = 6.56 μM | 24315192 | |||
| A375 | Function assay | IC50 = 6.599 μM | 21807507 | |||
| HCT116 | Function assay | GI50 = 6.6 μM | 15225706 | |||
| HepG2 | Cytotoxicity assay | IC50 = 6.7 μM | 26159483 | |||
| BCPAP | Antiproliferative activity assay | IC50 = 6.7 μM | 29032031 | |||
| A549 | Cytotoxicity assay | IC50 = 6.7 μM | 28865276 | |||
| PC3 | Cytotoxicity assay | IC50 = 6.8 μM | 23021967 | |||
| SGC7901 | Cytotoxicity assay | IC50 = 6.9 μM | 23454017 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 7 μM | 29517908 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 7 μM | 29297688 | |||
| COLO205 | Antiproliferative activity human | IC50 = 7.04 μM | 28242553 | |||
| rhabdomyosarcoma | Cytotoxicity activity against human | CC50 = 7.05 μM | 27288186 | |||
| HuH7 | Cytotoxicity assay | IC50 = 7.1 μM | 26159483 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 7.18 μM | 22721924 | |||
| FLT3-negative K562 | Cytotoxicity assay | GI50 = 7.3 μM | 23618709 | |||
| K562 | Function assay | GI50 = 7.3 μM | 26081023 | |||
| K562 | Function assay | GI50 = 7.3 μM | 26081023 | |||
| MCF7 | Antiproliferative activity assay | IC50 = 7.33 μM | 23644219 | |||
| A549 | Cytotoxicity assay | TGI = 7.36 μM | 26590508 | |||
| WI38 | Cytotoxicity assay | IC50 = 7.54 μM | 24826815 | |||
| A375 | Cytotoxicity assay | IC50 = 7.56 μM | 24215818 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 7.62 μM | 20181414 | |||
| 786-0 | Cytotoxicity assay | TGI = 7.62 μM | 26590508 | |||
| HS27 | Antiproliferative activity assay | IC50 = 7.8 μM | 19857963 | |||
| HS27 | Cytotoxicity assay | IC50 = 7.8 μM | 19897366 | |||
| HCT116 | Cytotoxicity assay | IC50 = 7.8 μM | 22483592 | |||
| HS27 | Antiproliferative activity assay | IC50 = 7.85 μM | 19464887 | |||
| HS27 | Antiproliferative activity assay | GI50 = 7.85 μM | 21353571 | |||
| A549/ATCC | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| DU145 | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| NCI/ADR-RES | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| MCF7 | Growth inhibition assay | TGI = 7.94 μM | 28088086 | |||
| PC3 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| UO31 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| NCI-ADR-RES | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| LOXIMVI | Antiproliferative activity assay | LC50 = 7.94 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| KM12 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| COLO205 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| NCI-H226 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| HOP62 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| T47D | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| MDA-MB-468 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| EKVX | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| MCF7 | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| Hs 578T | Antiproliferative activity assay | TGI = 7.94 μM | 27017549 | |||
| MGC803 | Antiproliferative activity assay | IC50 = 7.99 μM | 26560049 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 8.08 μM | 24440479 | |||
| PC3 | Cytotoxicity assay | IC50 = 8.08 μM | 27043268 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 8.08 μM | 23644219 | |||
| WM266.4 | Antiproliferative activity assay | GI50 = 8.1 μM | 23025996 | |||
| WM266.4 | Antiproliferative activity assay | GI50 = 8.12 μM | 22583669 | |||
| Ketr3 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| A375 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| MX1 | Antiproliferative activity assay | IC50 = 8.27 μM | 30216849 | |||
| MX1 | Cytotoxicity assay | IC50 = 8.27 μM | 24675135 | |||
| WM266.4 | Growth inhibition assay | GI50 = 8.3 μM | 22361686 | |||
| PLC/PRF/5 | Cytotoxicity assay | IC50 = 8.3 μM | 21531053 | |||
| A375 | Antiproliferative activity assay | IC50 = 8.33 μM | 29886324 | |||
| HCT116 | Cytotoxicity assay | IC50 = 8.41 μM | 29631788 | |||
| WI38 | Cytotoxicity assay | IC50 = 8.42 μM | 26991938 | |||
| HepG2 | Cytotoxicity assay | IC50 = 8.42 μM | 27162123 | |||
| HepG2 | Cytotoxicity assay | IC50 = 8.42 μM | 23871909 | |||
| HT-29 | Antiproliferative activity assay | IC50 = 8.44 μM | 29602674 | |||
| HepG2 | Cytotoxicity assay | IC50 = 8.67 μM | 24675135 | |||
| MCF7 | Cytotoxicity assay | IC50 = 8.83 μM | 20435479 | |||
| MCF7 | Cytotoxicity assay | IC50 = 9.12 μM | 24300920 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 9.14 μM | 26560049 | |||
| A375 | Cytotoxicity assay | IC50 = 9.17 μM | 24675135 | |||
| MGC803 | Antiproliferative activity assay | IC50 = 9.2 μM | 29032031 | |||
| SKOV3 | Cytotoxicity assay | IC50 = 9.25 μM | 24300920 | |||
| RS4:11 | Function assay | GI50 = 9.3 μM | 26081023 | |||
| RS4:11 | Cytotoxicity assay | GI50 = 9.3 μM | 23618709 | |||
| MIAPaCa2 | Antiproliferative activity assay | IC50 = 9.32 μM | 29032031 | |||
| PANC1 | Growth inhibition assay | IC50 = 9.32 μM | 29102175 | |||
| MHCC97H | Growth inhibition assay | IC50 = 9.32 μM | 29102175 | |||
| RS4:11 | Antiproliferative activity assay | GI50 = 9.4 μM | 21708468 | |||
| Hep3B | Cytotoxicity assay | IC50 = 9.4 μM | 28865276 | |||
| LoVo | Growth inhibition assay | IC50 = 9.47 μM | 29102175 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 9.96 μM | 25637123 | |||
| MCF7 | Cytotoxicity assay | TGI = 9.97 μM | 26590508 | |||
| IGROV1 | Growth inhibition assay | TGI = 10 μM | 28088086 | |||
| ACHN | Growth inhibition assay | TGI = 10 μM | 28088086 | |||
| TK10 | Growth inhibition assay | TGI = 10 μM | 28088086 | |||
| 786-0 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| SN12C | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| Caki1 | Antiproliferative activity assay | LC50 = 10 μM | 27017549 | |||
| TK10 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| RXF393 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| OVCAR8 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| SNB75 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| NCI-H322M | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| MDA-MB-435 | Antiproliferative activity assay | LC50 = 10 μM | 27017549 | |||
| SF539 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| SF268 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| NCI-H460 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| DU145 | Antiproliferative activity assay | TGI = 10 μM | 27017549 | |||
| K1 | Antiproliferative activity assay | IC50 = 10.2 μM | 29032031 | |||
| Bel7402 | Cytotoxicity assay | IC50 = 10.26 μM | 21504204 | |||
| Bel7402 | Growth inhibition assay | IC50 = 10.31 μM | 29102175 | |||
| OVCAR3 | Cytotoxicity assay | TGI = 10.32 μM | 26590508 | |||
| SGC7901 | Cytotoxicity assay | IC50 = 10.37 μM | 20435479 | |||
| SNB75 | Cytotoxicity assay | TGI = 10.42 μM | 26590508 | |||
| A431 | Antiproliferative activity assay | IC50 = 10.46 μM | 29032031 | |||
| SMMC7721 | Antiproliferative activity assay | IC50 = 10.61 μM | 29032031 | |||
| GES-1 | Cytotoxicity assay | IC50 = 10.68 μM | 27162123 | |||
| H460 | Cytotoxicity assay | IC50 = 10.8 μM | 24300920 | |||
| BGC823 | Antiproliferative activity assay | IC50 = 10.91 μM | 22721924 | |||
| Hep3B | Cytotoxicity assay | IC50 = 11.2 μM | 28342400 | |||
| MCF7 | Cytotoxicity assay | IC50 = 11.34 μM | 27162123 | |||
| MCF7 | Cytotoxicity assay | IC50 = 11.34 μM | 23871909 | |||
| SK-MEL-2 | Antiproliferative activity human | IC50 = 11.35 μM | 28242553 | |||
| HepG2 | Cytotoxicity assay | IC50 = 11.49 μM | 21504204 | |||
| A375P | Antiproliferative activity assay | IC50 = 11.5 μM | 22014559 | |||
| SGC7901 | Cytotoxicity assay | IC50 = 11.5 μM | 24300920 | |||
| HeLa | Antiproliferative activity assay | IC50 = 12.01 μM | 29103873 | |||
| PANC1 | Cytotoxicity assay | IC50 = 12.3 μM | 24300920 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 12.54 μM | 29032031 | |||
| A549 | Antiproliferative activity assay | IC50 = 12.54 μM | 23644219 | |||
| Caki1 | Growth inhibition assay | TGI = 12.59 μM | 28088086 | |||
| OVCAR8 | Growth inhibition assay | TGI = 12.59 μM | 28088086 | |||
| SKOV3 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| ACHN | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| OVCAR3 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| OVCAR4 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| HCT15 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| SW620 | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| A549/ATCC | Antiproliferative activity assay | TGI = 12.6 μM | 27017549 | |||
| MDA-MB-468 | Cytotoxicity assay | TGI = 13.09 μM | 26590508 | |||
| SK-MEL-28 | Cytotoxicity assay | TGI = 13.39 μM | 26590508 | |||
| A549 | Antiproliferative activity assay | IC50 = 13.64 μM | 26560049 | |||
| A375 | Antiproliferative activity human | IC50 = 13.64 μM | 28242553 | |||
| A375 | Antiproliferative activity assay | IC50 = 13.64 μM | 25462267 | |||
| K562 | Antiproliferative activity assay | IC50 = 13.85 μM | 23644219 | |||
| Hep3B | Cytotoxicity assay | IC50 = 14.08 μM | 21504204 | |||
| T47D | Cytotoxicity assay | TGI = 14.38 μM | 26590508 | |||
| NCI-H226 | Cytotoxicity assay | TGI = 14.42 μM | 26590508 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 14.62 μM | 24440479 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 14.62 μM | 23644219 | |||
| NCI-H522 | Cytotoxicity assay | TGI = 14.82 μM | 26590508 | |||
| SK-MEL-2 | Cytotoxicity assay | TGI = 14.85 μM | 26590508 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 15 μM | 29786436 | |||
| HepG2 | Antiproliferative activity assay | IC50 = 15 μM | 29103873 | |||
| fibroblast | Antiproliferative activity assay | IC50 = 15.1 μM | 18477505 | |||
| HT-29 | Cytotoxicity assay | IC50 = 15.2 μM | 24675135 | |||
| U87MG | Cytotoxicity assay | IC50 = 15.57 μM | 24826815 | |||
| BT549 | Antiproliferative activity assay | LC50 = 15.8 μM | 27017549 | |||
| GES-1 | Cytotoxicity assay | IC50 = 15.8 μM | 23871909 | |||
| SNB19 | Antiproliferative activity assay | TGI = 15.85 μM | 27017549 | |||
| IGROV1 | Antiproliferative activity assay | TGI = 15.9 μM | 27017549 | |||
| HCT116 | Antiproliferative activity assay | LC50 = 15.9 μM | 27017549 | |||
| OS-RC2 | Cytotoxicity assay | IC50 = 16 μM | 23454017 | |||
| A375 | Cytotoxicity assay | IC50 = 16.24 μM | 25461318 | |||
| SKOV3 | Cytotoxicity assay | TGI = 16.36 μM | 26590508 | |||
| WM1361 | Antiproliferative activity assay | IC50 = 16.44 μM | 29602674 | |||
| MKN28 | Antiproliferative activity assay | IC50 = 17 μM | 29032031 | |||
| SMMC7721 | Cytotoxicity assay | IC50 = 17.3 μM | 21504204 | |||
| UACC257 | Cytotoxicity assay | TGI = 17.33 μM | 26590508 | |||
| EAhy926 | Antiangiogenic activity assay | IC50 = 18.52 μM | 29032031 | |||
| SMMC7721 | Cytotoxicity assay | IC50 = 18.7 μM | 24300920 | |||
| Ketr3 | Cytotoxicity assay | IC50 = 18.8 μM | 24675135 | |||
| NCI-H522 | Cytotoxicity assay | IC50 = 19.26 μM | 25461318 | |||
| A549 | Cytotoxicity assay | IC50 = 19.54 μM | 27162123 | |||
| SH-SY5Y | Cytotoxicity assay | IC50 = 19.54 μM | 23871909 | |||
| MGC803 | Antiproliferative activity assay | IC50 = 19.92 μM | 29103873 | |||
| EKVX | Growth inhibition assay | TGI = 19.95 μM | 28088086 | |||
| OVCAR5 | Antiproliferative activity assay | TGI = 20 μM | 27017549 | |||
| UACC62 | Antiproliferative activity assay | LC50 = 20 μM | 27017549 | |||
| UACC257 | Antiproliferative activity assay | LC50 = 20 μM | 27017549 | |||
| MDA-MB-231 | Antiproliferative activity assay | LC50 = 20 μM | 27017549 | |||
| U87 | Cytotoxicity assay | IC50 = 21.07 μM | 20435479 | |||
| EJ | Cytotoxicity assay | IC50 = 22.9 μM | 24300920 | |||
| HCT116 | Antiproliferative activity assay | IC50 = 23.31 μM | 29602674 | |||
| HOP62 | Cytotoxicity assay | TGI = 23.55 μM | 26590508 | |||
| MDA-MB-231 | Cytotoxicity assay | TGI = 23.93 μM | 26590508 | |||
| PC3 | Antiproliferative activity assay | IC50 = 24.2 μM | 24440479 | |||
| PC3 | Antiproliferative activity assay | IC50 = 24.2 μM | 23644219 | |||
| EAhy926 | Antiproliferative activity assay | IC50 = 24.36 μM | 28068599 | |||
| EAhy926 | Anti-angiogenic activity in human | IC50 = 24.36 μM | 29102175 | |||
| U251 | Cytotoxicity assay | IC50 = 24.71 μM | 20435479 | |||
| NIH/3T3 | Antiproliferative activity assay | IC50 = 24.75 μM | 21592628 | |||
| NIH/3T3 | Antiproliferative activity assay | IC50 = 24.75 μM | 22647720 | |||
| DU145 | Cytotoxicity assay | IC50 = 24.91 μM | 27162123 | |||
| DU145 | Cytotoxicity assay | IC50 = 24.91 μM | 23871909 | |||
| U251 | Antiproliferative activity assay | LC50 = 25.1 μM | 27017549 | |||
| M14 | Antiproliferative activity assay | LC50 = 25.1 μM | 27017549 | |||
| NCI-H522 | Antiproliferative activity assay | LC50 = 25.1 μM | 27017549 | |||
| OVCAR4 | Growth inhibition assay | TGI = 25.12 μM | 28088086 | |||
| SH-SY5Y | Cytotoxicity assay | IC50 = 27.71 μM | 27162123 | |||
| A549 | Cytotoxicity assay | IC50 = 27.71 μM | 23871909 | |||
| PLC/PRF/5 | Cytotoxicity assay | IC50 = 29.9 μM | 28109948 | |||
| SK-MEL-5 | Cytotoxicity assay | TGI = 31.26 μM | 26590508 | |||
| A498 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| SK-MEL-28 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| KM12 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| COLO205 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| NCI-H226 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| SF295 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| HOP62 | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| T47D | Antiproliferative activity assay | LC50 = 31.6 μM | 27017549 | |||
| MHCC97L | Cytotoxicity assay | IC50 = 34.41 μM | 28109948 | |||
| MDA-MB-231 | Antiproliferative activity assay | IC50 = 35 μM | 24315192 | |||
| MDA-MB-231 | Cytotoxicity assay | IC50 = 36 μM | 22483592 | |||
| B16-BL6 | Cytotoxicity assay | IC50 = 36.48 μM | 29631788 | |||
| UO31 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SN12C | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| RXF393 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SNB75 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SF268 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| NCI-H23 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| HT-29 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| HOP92 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| NCI-H460 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| SW620 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| MDA-MB-468 | Antiproliferative activity assay | LC50 = 39.8 μM | 27017549 | |||
| MALME-3M | Growth inhibition assay | TGI = 39.81 μM | 28088086 | |||
| Klik om meer experimentele gegevens over de cellijn te bekijken | ||||||
| Moleculair gewicht | 464.82 | Formule | C21H16ClF3N4O3 |
Opslag (Vanaf de ontvangstdatum) | |
|---|---|---|---|---|---|
| CAS-nr. | 284461-73-0 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | NSC-724772,BAY 43-9006 | Smiles | CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F | ||
|
In vitro |
DMSO
: 92 mg/mL
(197.92 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
Raf-1
(Cell-free assay) 6 nM
mVEGFR2(Flk1)
(Cell-free assay) 15 nM
mVEGFR3
(Cell-free assay) 20 nM
B-Raf
(Cell-free assay) 22 nM
B-Raf (V599E)
(Cell-free assay) 38 nM
mPDGFRβ
(Cell-free assay) 57 nM
FLT3
(Cell-free assay) 58 nM
c-Kit
(Cell-free assay) 68 nM
VEGFR2
(Cell-free assay) 90 nM
FGFR1
(Cell-free assay) 580 nM
|
|---|---|
| In vitro |
Sorafenib remt zowel wild-type als V599E-mutant B-Raf-activiteit met een IC50 van respectievelijk 22 nM en 38 nM. Deze verbinding remt ook potent mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3 en c-Kit met een IC50 van respectievelijk 15 nM, 20 nM, 57 nM, 58 nM en 68 nM. Het remt zwak FGFR-1 met een IC50 van 580 nM. Deze chemische stof is niet actief tegen ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ en pim-1. Het remt significant VEGFR2-fosforylering in NIH 3T3-cellen met een IC50 van 30 nM en Flt-3-fosforylering in HEK-293-cellen met een IC50 van 20 nM. Dit middel blokkeert potent MEK 1/2- en ERK 1/2-fosforylering in de meeste cellijnen, maar niet in A549- of H460-cellen, terwijl het geen effect heeft op de remming van de PKB-pathway. Het remt de proliferatie van HAoSMC- en MDA-MB-231-cellen met een IC50 van respectievelijk 0,28 μM en 2,6 μM. Naast de remming van de RAF/MEK/ERK-signaleringspathway remt deze verbinding de fosforylering van eIF4E significant en downreguleert Mcl-1-niveaus in hepatocellulaire carcinoom (HCC)-cellen op een MEK/ERK-onafhankelijke manier. Het remt de proliferatie van PLC/PRF/5- en HepG2-cellen met een IC50 van respectievelijk 6,3 μM en 4,5 μM, en leidt tot een significante inductie van apoptosis.
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| Kinase Assay |
Biochemische assays
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|
Recombinant baculovirussen die Raf-1 (residuen 305-648) en B-Raf (residuen 409-765) tot expressie brengen, worden gezuiverd als fusie-eiwitten. Volledig menselijk MEK-1 wordt gegenereerd door PCR en gezuiverd als een fusie-eiwit uit Escherichia coli-lysaten. Sorafenib-tosylaat wordt toegevoegd aan een mengsel van Raf-1 (80 ng), of B-Raf (80 ng) met MEK-1 (1 μg) in assaybuffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, en 0,15% β-mercaptoethanol] met een eindconcentratie van 1% DMSO. De Raf-kinaseassay (eindvolume van 50 μL) wordt geïnitieerd door 25 μL 10 μM γ[33P]ATP (400 Ci/mol) toe te voegen en geïncubeerd bij 32 °C gedurende 25 minuten. Gefosforyleerd MEK-1 wordt geoogst door filtratie op een fosfocellulosemat, en 1% fosforzuur wordt gebruikt om ongebonden radioactiviteit weg te wassen. Na drogen door microgolfverwarming wordt een β-plaatcounter gebruikt om filtergebonden radioactiviteit te kwantificeren. Humaan VEGFR2 (KDR) kinase domein wordt tot expressie gebracht en gezuiverd uit Sf9-lysaten. Tijdsopgeloste fluorescentie-energieoverdrachtsassays voor VEGFR2 worden uitgevoerd in 96-well ondoorzichtige platen in het tijdsopgeloste fluorescentie-energieoverdrachtsformaat. De uiteindelijke reactiecondities zijn als volgt: 1 tot 10 μM ATP, 25 nM poly GT-biotine, 2 nM Europium-gelabeld phospho (p)-Tyr antilichaam (PY20), 10 nM APC, 1 tot 7 nM cytoplasmatisch kinase domein in eindconcentraties van 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0,1 mM EDTA, 0,015% Brij-35, 0,1 mg/mL BSA, en 0,1% β-mercaptoethanol. Reactievolumes zijn 100 μL en worden geïnitieerd door toevoeging van enzym. Platen worden gelezen bij zowel 615 als 665 nM op een Perkin-Elmer VictorV Multilabel counter op ~1,5 tot 2,0 uur na initiatie van de reactie. Signaal wordt berekend als een verhouding: (665 nm/615 nM) × 10.000 voor elke well. Voor IC50-generatie wordt deze verbinding toegevoegd vóór de enzyminitiatie. Een 50-voudige stockplaat wordt gemaakt met deze verbinding serieel verdund 1:3 in een 50% DMSO/50% gedestilleerd water oplossing. De eindconcentraties van deze chemische stof variëren van 10 μM tot 4,56 nM in 1% DMSO.
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| In vivo |
Orale toediening van Sorafenib (~60 mg/kg) toont een breed spectrum, dosisafhankelijke antitumoractiviteit tegen verschillende menselijke tumortransplantaatmodellen, waaronder MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460 en A549, zonder bewijs van toxiciteit. In samenhang met de antitumorwerkzaamheid remt deze verbinding de MEK 1/2-fosforylering en pERK 1/2-niveaus potent in HT-29 en MDA-MB-231-xenografts, maar niet in Colo-205-xenografts, en onderdrukt het significant het tumor-microvatgebied (MVA) en de microvatdichtheid (MVD) in MDA MB-231, HT-29 en Colo-205-tumortransplantaten. Dit middel produceert dosisafhankelijke groeiremming van PLC/PRF/5-tumortransplantaten in SCID-muizen met TGI's van 49% en 78% bij respectievelijk 10 mg/kg en 30 mg/kg, consistent met de remming van ERK- en eIF4E-fosforylering, vermindering van het microvatgebied en inductie van tumorcelapoptosis. Het sensibiliseert bax-/--cellen voor TRAIL op een dosisafhankelijke manier, via een mechanisme dat de downregulatie van NF-κB-gemedieerde Mcl-1- en cIAP2-expressie omvat. Het combineren van deze verbinding (30-60 mg/kg) met TRAIL (5 mg/kg) toont dramatische werkzaamheid in TRAIL-resistente HCT116 bax-/- en HT29-tumortransplantaten.
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Referenties |
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| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | LC3-I / LC-3II / ATG5 p-STAT3 / STAT3 / Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1 |
|
23392173 |
| Growth inhibition assay | Cell viability |
|
26039995 |
| Immunofluorescence | p65 cytochrome c |
|
22286758 |
| ELISA | TGF-beta / CD206 Caspase-9 / Caspase-3 |
|
26158762 |
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Rekrutering | Aandoeningen | Sponsor/Medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT05068752 | Recruiting | Pancreas Cancer |
HonorHealth Research Institute|Bayer|Genentech Inc. |
October 28 2021 | Phase 2 |
| NCT04763408 | Active not recruiting | Carcinoma Hepatocellular |
Eisai Inc. |
April 9 2021 | -- |
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