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SKI-606 (Bosutinib) Src/Abl-remmer
Cat.nr.S1014
Chemische structuur
Molecuulgewicht: 530.45
Spring naar
Kwaliteitscontrole
Batch:
Zuiverheid:
99.94%
99.94
| Gerelateerde doelwitten | EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Overig Src Inhibitoren | WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466 |
Celkweek, behandeling & werkzame concentratie
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| NB7 | Growth Inhibition Assay | IC50=0.08231 μM | SANGER | |||
| SW756 | Growth Inhibition Assay | IC50=0.14024 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=0.16398 μM | SANGER | |||
| HSC-4 | Growth Inhibition Assay | IC50=0.17158 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.28664 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.34068 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=0.35216 μM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=0.37786 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=0.40808 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.41576 μM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=0.43464 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.4389 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=0.44108 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=0.45633 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=0.4659 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=0.48572 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=0.48584 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=0.48797 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=0.49509 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.50792 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.51214 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.53718 μM | SANGER | |||
| ACHN | Growth Inhibition Assay | IC50=0.54069 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=0.5482 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=0.55349 μM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=0.55465 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=0.55935 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=0.67498 μM | SANGER | |||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.7233 μM | SANGER | |||
| SW13 | Growth Inhibition Assay | IC50=0.73798 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=0.79208 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=0.83104 μM | SANGER | |||
| OC-314 | Growth Inhibition Assay | IC50=0.86965 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=0.90675 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.92466 μM | SANGER | |||
| CAL-27 | Growth Inhibition Assay | IC50=0.92906 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.97248 μM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=1.00394 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=1.0165 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=1.05017 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=1.0881 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.09058 μM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=1.11783 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=1.13351 μM | SANGER | |||
| 5637 | Growth Inhibition Assay | IC50=1.13803 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=1.19302 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=1.2079 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=1.22892 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=1.23785 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=1.24255 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.26106 μM | SANGER | |||
| HO-1-N-1 | Growth Inhibition Assay | IC50=1.26369 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=1.28714 μM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=1.29205 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=1.29356 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=1.30704 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=1.31383 μM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=1.31775 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=1.40113 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=1.41273 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=1.43657 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=1.43973 μM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=1.44805 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=1.4936 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=1.51722 μM | SANGER | |||
| A375 | Growth Inhibition Assay | IC50=1.51772 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=1.55007 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=1.5626 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=1.57155 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=1.61804 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=1.63584 μM | SANGER | |||
| HT-1376 | Growth Inhibition Assay | IC50=1.6436 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=1.65709 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=1.67551 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=1.6892 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=1.69596 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=1.69856 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=1.71802 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=1.74599 μM | SANGER | |||
| KYSE-140 | Growth Inhibition Assay | IC50=1.75655 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=1.86747 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=1.89849 μM | SANGER | |||
| HN | Growth Inhibition Assay | IC50=1.89874 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=1.93628 μM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=1.97679 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=1.99325 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=1.99888 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.00435 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition Assay | IC50=2.00745 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=2.03372 μM | SANGER | |||
| MEL-JUSO | Growth Inhibition Assay | IC50=2.04464 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=2.07058 μM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=2.09889 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=2.13458 μM | SANGER | |||
| CAL-39 | Growth Inhibition Assay | IC50=2.1448 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=2.18973 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=2.22984 μM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=2.26824 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=2.30909 μM | SANGER | |||
| FADU | Growth Inhibition Assay | IC50=2.32296 μM | SANGER | |||
| A431 | Growth Inhibition Assay | IC50=2.37025 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=2.38019 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=2.40417 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=2.42869 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=2.43507 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=2.66391 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=2.71406 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=2.73164 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=2.7431 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=2.76673 μM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=2.78224 μM | SANGER | |||
| COR-L23 | Growth Inhibition Assay | IC50=2.79464 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=2.80161 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=2.81638 μM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=2.85003 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=2.89243 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=2.99415 μM | SANGER | |||
| EPLC-272H | Growth Inhibition Assay | IC50=3.00235 μM | SANGER | |||
| 8505C | Growth Inhibition Assay | IC50=3.10301 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=3.14277 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=3.14706 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=3.17263 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=3.18418 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=3.20117 μM | SANGER | |||
| T-24 | Growth Inhibition Assay | IC50=3.21814 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=3.22232 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition Assay | IC50=3.24829 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=3.25486 μM | SANGER | |||
| ME-180 | Growth Inhibition Assay | IC50=3.26051 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=3.2901 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=3.2913 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=3.30172 μM | SANGER | |||
| GMS-10 | Growth Inhibition Assay | IC50=3.34086 μM | SANGER | |||
| SCH | Growth Inhibition Assay | IC50=3.40844 μM | SANGER | |||
| C-33-A | Growth Inhibition Assay | IC50=3.41421 μM | SANGER | |||
| NCI-H1703 | Growth Inhibition Assay | IC50=3.41812 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=3.46124 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=3.48199 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=3.49802 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=3.5729 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=3.58569 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=3.58829 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=3.64122 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=3.64276 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=3.67854 μM | SANGER | |||
| HuCCT1 | Growth Inhibition Assay | IC50=3.74177 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=3.96971 μM | SANGER | |||
| KYSE-450 | Growth Inhibition Assay | IC50=3.96997 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=3.9729 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=3.97481 μM | SANGER | |||
| Mewo | Growth Inhibition Assay | IC50=4.06361 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=4.09799 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=4.10501 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=4.16739 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=4.18695 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=4.23333 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=4.24571 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=4.29141 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=4.34244 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=4.37355 μM | SANGER | |||
| M14 | Growth Inhibition Assay | IC50=4.48792 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=4.5012 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=4.53612 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=4.53924 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=4.59559 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=4.61261 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=4.62411 μM | SANGER | |||
| KYSE-270 | Growth Inhibition Assay | IC50=4.65126 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=4.71291 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=4.81379 μM | SANGER | |||
| MKN1 | Growth Inhibition Assay | IC50=4.83914 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=4.85626 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=4.9298 μM | SANGER | |||
| G-361 | Growth Inhibition Assay | IC50=5.01003 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=5.03291 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=5.04038 μM | SANGER | |||
| HuP-T4 | Growth Inhibition Assay | IC50=5.14334 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=5.3428 μM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=5.37682 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=5.41585 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=5.44212 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=5.45986 μM | SANGER | |||
| Ca-Ski | Growth Inhibition Assay | IC50=5.46115 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=5.54925 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=5.58938 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=5.61486 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=5.69091 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=5.72685 μM | SANGER | |||
| PA-1 | Growth Inhibition Assay | IC50=5.81893 μM | SANGER | |||
| HCC1937 | Growth Inhibition Assay | IC50=5.83929 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=5.91121 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=6.0517 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=6.07797 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=6.09261 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=6.13501 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=6.16115 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=6.17993 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=6.18081 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=6.18082 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=6.21816 μM | SANGER | |||
| T47D | Growth Inhibition Assay | IC50=6.26457 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=6.37701 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=6.43561 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=6.97043 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=7.1641 μM | SANGER | |||
| KU-19-19 | Growth Inhibition Assay | IC50=7.16476 μM | SANGER | |||
| MKN45 | Growth Inhibition Assay | IC50=7.18699 μM | SANGER | |||
| SCC-25 | Growth Inhibition Assay | IC50=7.23414 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=7.25514 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=7.29319 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=7.32492 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=7.32506 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=7.37651 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=7.38278 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=7.38473 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=7.41458 μM | SANGER | |||
| CHP-212 | Growth Inhibition Assay | IC50=7.51896 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=7.59066 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=7.70312 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=7.72258 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=7.82172 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=7.9906 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=8.0407 μM | SANGER | |||
| KYSE-180 | Growth Inhibition Assay | IC50=8.08648 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=8.11057 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=8.25496 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition Assay | IC50=8.28364 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=8.28397 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=8.44465 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=8.59774 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=8.66597 μM | SANGER | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=8.77625 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=8.83001 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=8.83101 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition Assay | IC50=8.84157 μM | SANGER | |||
| RCM-1 | Growth Inhibition Assay | IC50=9.08145 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=9.12028 μM | SANGER | |||
| HCC1395 | Growth Inhibition Assay | IC50=9.30896 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=9.36026 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=9.65534 μM | SANGER | |||
| HCC1954 | Growth Inhibition Assay | IC50=9.85859 μM | SANGER | |||
| NCI-H1838 | Growth Inhibition Assay | IC50=9.90371 μM | SANGER | |||
| SW620 | Growth Inhibition Assay | IC50=9.95357 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=10.4197 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=10.4248 μM | SANGER | |||
| NCI-H1666 | Growth Inhibition Assay | IC50=10.4355 μM | SANGER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=10.4753 μM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=10.6396 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=10.8004 μM | SANGER | |||
| RVH-421 | Growth Inhibition Assay | IC50=11.152 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=11.2478 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=11.3833 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=11.7319 μM | SANGER | |||
| BEN | Growth Inhibition Assay | IC50=11.7402 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=11.9091 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=12.0666 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=12.0893 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=12.4472 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=12.5506 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=12.7307 μM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=12.7455 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=12.7713 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=12.8046 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=12.8212 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=12.8874 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=13.0267 μM | SANGER | |||
| SW626 | Growth Inhibition Assay | IC50=13.2485 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=13.2512 μM | SANGER | |||
| NCI-H2029 | Growth Inhibition Assay | IC50=13.8108 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=13.9927 μM | SANGER | |||
| HMV-II | Growth Inhibition Assay | IC50=14.078 μM | SANGER | |||
| EW-22 | Growth Inhibition Assay | IC50=14.1502 μM | SANGER | |||
| AsPC-1 | Growth Inhibition Assay | IC50=14.564 μM | SANGER | |||
| COLO-678 | Growth Inhibition Assay | IC50=14.7271 μM | SANGER | |||
| HCT-15 | Growth Inhibition Assay | IC50=14.8855 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=14.8874 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=15.0643 μM | SANGER | |||
| AU565 | Growth Inhibition Assay | IC50=15.2096 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=15.2681 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=15.4412 μM | SANGER | |||
| 23132-87 | Growth Inhibition Assay | IC50=15.8495 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=15.9636 μM | SANGER | |||
| KYSE-410 | Growth Inhibition Assay | IC50=16.029 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=16.062 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=16.1823 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=16.1916 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=16.25 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=16.4143 μM | SANGER | |||
| COLO-680N | Growth Inhibition Assay | IC50=16.5108 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=16.9893 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=17.1535 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=17.1701 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=17.2066 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=17.4832 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=17.6285 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=17.6629 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=17.8149 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=17.8294 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=18.0183 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=18.0577 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition Assay | IC50=18.1021 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=18.2918 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=18.5929 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=18.6702 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=18.7997 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=18.8331 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=18.9164 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=19.0877 μM | SANGER | |||
| U031 | Growth Inhibition Assay | IC50=19.4909 μM | SANGER | |||
| FTC-133 | Growth Inhibition Assay | IC50=19.9304 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=20.3761 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=20.4699 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=21.3926 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=21.485 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=21.8451 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=22.1022 μM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=22.1603 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=22.2907 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=22.434 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=22.7045 μM | SANGER | |||
| DoTc2-4510 | Growth Inhibition Assay | IC50=23.6472 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=23.6911 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=23.7939 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=24.146 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=24.242 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=24.4024 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=25.0235 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=25.2062 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=25.2993 μM | SANGER | |||
| BFTC-909 | Growth Inhibition Assay | IC50=25.3551 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=25.6744 μM | SANGER | |||
| SW1990 | Growth Inhibition Assay | IC50=25.9655 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=26.0443 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=26.0668 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=26.1574 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=26.5317 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=27.7479 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=27.7694 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=28.1229 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=28.2218 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=28.2762 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=28.3566 μM | SANGER | |||
| BT-20 | Growth Inhibition Assay | IC50=28.3685 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=28.4838 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=28.779 μM | SANGER | |||
| SW837 | Growth Inhibition Assay | IC50=29.3385 μM | SANGER | |||
| 647-V | Growth Inhibition Assay | IC50=29.7003 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=29.8013 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=30.0733 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=30.6093 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=31.3629 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=32.4317 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=33.0251 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=33.0354 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=33.2535 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=33.4285 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=34.1408 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=35.0729 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=35.1553 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=36.5902 μM | SANGER | |||
| OE33 | Growth Inhibition Assay | IC50=37.7577 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=38.5267 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=38.7428 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=39.0471 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=39.7792 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=39.839 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=40.3604 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=41.5039 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=42.7263 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=42.8517 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=43.0483 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=43.6809 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=43.8776 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=43.9006 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=44.8017 μM | SANGER | |||
| PC-3 | Growth Inhibition Assay | IC50=45.8023 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=45.9889 μM | SANGER | |||
| SW1116 | Growth Inhibition Assay | IC50=47.0182 μM | SANGER | |||
| ZR-75-30 | Growth Inhibition Assay | IC50=47.0239 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=47.0918 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=47.6249 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=48.3529 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=49.1742 μM | SANGER | |||
| OE19 | Growth Inhibition Assay | IC50=49.2902 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition Assay | IC50=49.6861 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=49.9084 μM | SANGER | |||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0043 μM. | 26814890 | ||
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0127 μM. | 29941193 | ||
| fibroblast cells | Antiproliferative assay | Antiproliferative activity against Src-transformed rat2 fibroblast cells, IC50 = 0.1 μM. | 17181170 | |||
| fibroblast cells | Function assay | Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA, IC50 = 0.1 μM. | 17905586 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.128 μM. | 30137981 | ||
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.133 μM. | 29941193 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.14 μM. | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.146 μM. | 30137981 | ||
| Ba/F3 | Function assay | Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay, IC50 = 0.15 μM. | 16970400 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.177 μM. | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.195 μM. | 30137981 | ||
| Ba/F3 | Antiproliferative assay | Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50 = 0.2 μM. | 16970400 | |||
| Ba/F3 | Function assay | Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay, IC50 = 0.2 μM. | 16970400 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.204 μM. | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.243 μM. | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.278 μM. | 30137981 | ||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.356 μM. | 30137981 | ||
| fibroblast cells | Function assay | Inhibitory concentration against Abl transformed rat fibroblast cells, IC50 = 0.49 μM. | 16161995 | |||
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.642 μM. | 30137981 | ||
| Ba/F3 | Antiproliferative assay | Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50 = 1 μM. | 16970400 | |||
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.15 μM. | 18485715 | ||
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.17 μM. | 18485715 | ||
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 3.2 μM. | 26814890 | ||
| HeLa | Function assay | 4.5 hrs | Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 3.85 μM. | 29624387 | ||
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.87 μM. | 18485715 | ||
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.91 μM. | 18485715 | ||
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, TGI = 6.5 μM. | 18485715 | ||
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, TGI = 7.66 μM. | 18485715 | ||
| Ba/F3 | Cell death assay | Induction of cell death of murine BaF3 cells expressing NPM/ALK L256T mutant by trypan blue exclusion assay | 16970400 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
Chemische informatie, opslag en stabiliteit
| Molecuulgewicht | 530.45 | Formule | C26H29Cl2N5O3 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 380843-75-4 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | SKI-606 | Smiles | CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC | ||
Oplosbaarheid
|
In vitro |
DMSO
: 100 mg/mL
(188.51 mM)
Water : Insoluble Ethanol : Insoluble |
Molariteitscalculator
Verdunningscalculator
Molecuulgewichtcalculator
|
In vivo |
|||||
In vivo formulatiecalculator (heldere oplossing)
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
mg/kg
g
μL
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 de sectie oplosbaarheid.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
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. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
Werkingsmechanisme
| Targets/IC50/Ki |
S6 kinase
ERK
STAT3
LCK
Abl
(Cell-free assay) 1 nM
Src
(Cell-free assay) 1.2 nM
|
|---|---|
| In vitro |
Bosutinib is selectief voor Src boven niet-Src-familiekinasen met een IC50 van 1,2 nM, en remt potent Src-afhankelijke celproliferatie met een IC50 van 100 nM. Deze verbinding remt significant de proliferatie van Bcr-Abl-positieve leukemiecellijnen KU812, K562 en MEG-01, maar niet Molt-4, HL-60, Ramos en andere leukemiecellijnen, met respectievelijk IC50 van 5 nM, 20 nM en 20 nM, krachtiger dan die van STI-571. Vergelijkbaar met STI-571, vertoont het antiproliferatieve activiteit tegen de Abl-MLV-getransformeerde fibroblasten met IC50 van 90 nM. Deze chemische stof ablateert tyrosinefosforylering van Bcr-Abl en STAT5 in CML-cellen en van v-Abl uitgedrukt in fibroblasten bij een concentratie van ~50 nM, 10-25 nM en 200 nM, respectievelijk, wat leidt tot de Bcr-Abl stroomafwaartse signaalremming van Lyn/Hck-fosforylering. Hoewel het de proliferatie en overleving van borstkankercellen niet kan remmen, vermindert het significant de motiliteit en invasie van borstkankercellen met IC50 van ~250 nM, wat gepaard gaat met een toename van cel-celadhesie en membraanlokalisatie van β-catenine. |
| Kinase Assay |
De Src- en Abl-kinase-assays
|
|
De Src-kinase-activiteit wordt gemeten in een ELISA-formaat. Src (3 eenheden/reactie), reactiebuffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) en cdc2-substraatpeptide worden toegevoegd aan verschillende concentraties Bosutinib en geïncubeerd bij 30 °C gedurende 10 minuten. De reactie wordt gestart door de toevoeging van ATP tot een finale concentratie van 100 μM, geïncubeerd bij 30 °C gedurende 1 uur en gestopt door de toevoeging van EDTA. De instructies van de fabrikant worden gevolgd voor de daaropvolgende stappen. De Abl-kinase-assay wordt uitgevoerd in een DELFIA solid phase europium-gebaseerd detectieassay-formaat. Gebiotinyleerd peptide (2 μM) wordt gebonden aan met streptavidine gecoate microtiterplaten gedurende 1,5 uur in 1 mg/mL ovalbumine in PBS. De platen worden 1 uur gewassen met PBS/0.1% Tween 80, gevolgd door een PBS-was. De kinasereactie wordt 1 uur geïncubeerd bij 30°C. Abl-kinase (10 eenheden) wordt gemengd met 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumine en verschillende concentraties van deze verbinding. De reactie wordt gestopt met EDTA in een finale concentratie van 50 mM. De reactie wordt gemonitord met Eu-gelabelde fosfotyrosine-antilichaam en DELFIA-versterkingsoplossing.
|
|
| In vivo |
Bosutinib (60 mg/kg/dag) is actief tegen Src-getransformeerde fibroblast xenografts en HT29 xenografts in naakte muizen met een T/C van respectievelijk 18% en 30%. Orale toediening van deze verbinding gedurende 5 dagen onderdrukt significant de K562 tumorgroei bij muizen op een dosisafhankelijke manier, waarbij de grote tumoren werden uitgeroeid bij een dosis van 100 mg/kg en tumoren vrij waren bij 150 mg/kg zonder duidelijke toxiciteit. Aangezien het inactief is tegen Colo205 xenografts in naakte muizen bij 50 mg/kg tweemaal daags, is deze chemische dosering van 75 mg/kg tweemaal daags nodig tegen Colo205 xenografts, en het verhogen van de dosis van deze verbinding heeft geen extra voordeel, in tegenstelling tot het significante dosisafhankelijke vermogen tegen HT29 xenografts. |
Referenties |
|
Toepassingen
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | p-ABL / ABL p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3 |
|
28199182 |
| Immunofluorescence | p-FAK / p-STAT3 / beta-catenin |
|
18483306 |
| Growth inhibition assay | IC50 Cell viability |
|
27903968 |
Informatie over klinische proeven
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT05363488 | Completed | Myeloid Leukemia |
Pfizer |
October 8 2021 | -- |
| NCT04258943 | Active not recruiting | Philadelphia Chromosome Positive CML|Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Phase Chronic Myelogenous Leukemia |
Children''s Oncology Group|Erasmus Medical Center|Dutch Childhood Oncology Group|Innovative Therapies for Children with Cancer|Pfizer |
April 6 2020 | Phase 1|Phase 2 |
| NCT03023319 | Completed | Carcinoma Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer |
Nagla Abdel Karim|Augusta University |
December 10 2019 | Phase 1 |
| NCT03888222 | Completed | Dementia With Lewy Bodies |
Georgetown University|Alzheimer''s Association |
April 23 2019 | Phase 2 |
| NCT03854903 | Active not recruiting | Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer |
Georgetown University|Pfizer |
April 1 2019 | Phase 1 |
Technische ondersteuning
Tel: +1-832-582-8158 Ext:3
Als u nog andere vragen heeft, laat dan een bericht achter.
Veelgestelde vragen
Vraag 1:
Can I give S1014 to mice by oral gavage? If so, how to dissolve it?
Antwoord:
For oral gavage, it can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.
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