alleen voor onderzoeksdoeleinden
PD173074 FGFR1-remmer
Cat.nr.S1264
Chemische structuur
Molecuulgewicht: 523.67
Spring naar
Kwaliteitscontrole
Batch:
Zuiverheid:
99.95%
99.95
| Gerelateerde doelwitten | EGFR VEGFR JAK PDGFR Src HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Overig FGFR Inhibitoren | AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 Zoligratinib (Debio-1347) H3B-6527 Fisogatinib (BLU-554) SSR128129E Ferulic Acid |
Celkweek, behandeling & werkzame concentratie
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| NCI-H1581 | Growth Inhibition Assay | IC50=0.01225 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=0.05129 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=0.21576 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.32984 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=0.33898 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=0.34715 μM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=0.40133 μM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=0.54653 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=0.54701 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=0.56289 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=0.71159 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=0.78988 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.84623 μM | SANGER | |||
| MFE-280 | Growth Inhibition Assay | IC50=0.85872 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=1.24464 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=1.33886 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=1.36737 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=1.47378 μM | SANGER | |||
| DU-145 | Growth Inhibition Assay | IC50=1.58217 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=1.70355 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=2.094 μM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=2.14306 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=2.18394 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=2.21283 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=2.37939 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=2.47189 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=2.48364 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=2.65331 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.70747 μM | SANGER | |||
| MG-63 | Growth Inhibition Assay | IC50=2.94262 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=3.03472 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=3.12727 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=3.13564 μM | SANGER | |||
| RH-18 | Growth Inhibition Assay | IC50=3.19598 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=3.1969 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=3.23447 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=3.46576 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=3.47676 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=3.49855 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=3.50488 μM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=3.63969 μM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=3.65799 μM | SANGER | |||
| LK-2 | Growth Inhibition Assay | IC50=3.67133 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=3.67873 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=3.80051 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=3.83637 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=3.92075 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=3.92245 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=3.98923 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=4.28723 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=4.31534 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=4.41746 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=4.46817 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=4.5331 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=4.5481 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=4.55222 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=4.58283 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=4.87168 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=4.96665 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=5.2406 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=5.38843 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=5.72927 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=5.95032 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=6.21406 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=6.24977 μM | SANGER | |||
| CHP-134 | Growth Inhibition Assay | IC50=6.25182 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=6.41733 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=6.72671 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=6.73142 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=6.76626 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=6.91784 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=7.07764 μM | SANGER | |||
| ME-180 | Growth Inhibition Assay | IC50=7.10404 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=7.37819 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=7.48341 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=7.69626 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=8.11504 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=8.48149 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=8.50981 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=8.52212 μM | SANGER | |||
| NCI-H520 | Growth Inhibition Assay | IC50=8.62157 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=8.69786 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=8.75143 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=9.06534 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=9.09607 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=9.29526 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=9.35134 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=9.50595 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=9.89055 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=9.94534 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=9.97659 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=10.1393 μM | SANGER | |||
| SW948 | Growth Inhibition Assay | IC50=10.1882 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=10.5267 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=10.6576 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=10.7391 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=10.8901 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=11.0308 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=11.0737 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=11.2084 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=11.3837 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=11.4456 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=11.4947 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=11.6167 μM | SANGER | |||
| MKN45 | Growth Inhibition Assay | IC50=11.7993 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=11.9692 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=12.0346 μM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=12.3845 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=12.5295 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=12.791 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=13.0835 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=13.2704 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=13.3187 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=13.4195 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=13.4547 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=13.5318 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=13.8109 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=13.9868 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=14.4453 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=14.6676 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=15.1286 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=15.3869 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=15.9094 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=15.9107 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=15.9376 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=16.088 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=16.3384 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=16.5165 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=16.5889 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=16.9879 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=17.3391 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=17.7127 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=17.9307 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=17.975 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=18.1788 μM | SANGER | |||
| HCC1395 | Growth Inhibition Assay | IC50=18.4301 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=18.6388 μM | SANGER | |||
| NY | Growth Inhibition Assay | IC50=19.0809 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=19.1252 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=19.3952 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=19.7612 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=19.8852 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=19.962 μM | SANGER | |||
| HCC1569 | Growth Inhibition Assay | IC50=20.2624 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=20.2847 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=20.9808 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=21.3597 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=21.529 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=21.6172 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=22.6677 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=22.7601 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=23.0651 μM | SANGER | |||
| NCI-H596 | Growth Inhibition Assay | IC50=23.8527 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=24.2759 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=24.4045 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=25.0323 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=25.1061 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=25.3908 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=25.4319 μM | SANGER | |||
| FTC-133 | Growth Inhibition Assay | IC50=25.8186 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=26.296 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=26.4123 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=26.8145 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=28.2297 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=28.2399 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=28.4 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=28.4386 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=28.941 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=29.4557 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=29.5786 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=29.6472 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=29.7607 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=29.8807 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=29.8865 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=30.0933 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=30.1426 μM | SANGER | |||
| ESS-1 | Growth Inhibition Assay | IC50=30.4759 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=30.764 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=31.0897 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=31.1111 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=31.3296 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=31.361 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=31.8137 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=31.9243 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=32.0171 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=32.6884 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=32.9079 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=33.1005 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=33.275 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=33.3192 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=33.4307 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=33.4768 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=33.5551 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=33.5725 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=34.0335 μM | SANGER | |||
| MDA-MB-453 | Growth Inhibition Assay | IC50=34.6395 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=34.7181 μM | SANGER | |||
| SW900 | Growth Inhibition Assay | IC50=34.8115 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=35.1529 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=35.6061 μM | SANGER | |||
| OVCAR-3 | Growth Inhibition Assay | IC50=36.2045 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=36.2294 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=36.4699 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=37.4027 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=38.3433 μM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=38.3711 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=38.7158 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=38.9828 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=39.2502 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=39.385 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=39.9643 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=40.0764 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=40.1295 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=40.9783 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=40.9799 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition Assay | IC50=41.0926 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=42.2641 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=42.4368 μM | SANGER | |||
| LU-135 | Growth Inhibition Assay | IC50=42.5447 μM | SANGER | |||
| ZR-75-30 | Growth Inhibition Assay | IC50=43.0493 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=43.2679 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=43.7816 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=43.9534 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=43.9609 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=44.0533 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=44.5633 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=44.6105 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=44.9328 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=44.9868 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=45.6368 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=45.9217 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=46.321 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=46.4255 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=46.5709 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=47.547 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=47.683 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=47.727 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=48.1152 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=48.1853 μM | SANGER | |||
| KP-N-YN | Growth Inhibition Assay | IC50=48.2102 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=48.2726 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=48.2991 μM | SANGER | |||
| SUM52 | Antiproliferative assay | 5 days | Antiproliferative activity against human FGFR2-amplified SUM52 cells after 5 days by SRB assay, IC50 = 0.0123 μM. | 28521156 | ||
| RT112 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RT112 cells after 72 hrs by MTT assay, GI50 = 0.015 μM. | 27599742 | ||
| insect cells | Function assay | 10 mins | Inhibition of recombinant full length human FGFR1 expressed in baculovirus infected insect cells in presence of [gamma-32P]ATP after 10 mins by scintillation counting based radioactive filter binding assay, IC50 = 0.0215 μM. | 27914362 | ||
| SW780 | Antiproliferative assay | 5 days | Antiproliferative activity against human FGFR3-amplified SW780 cells after 5 days by SRB assay, IC50 = 0.0843 μM. | 28521156 | ||
| NIH/ 3T3 | Function assay | 5 mins | Inhibition of VEGFR2 (unknown origin) overexpressed in mouse NIH/ 3T3 cells incubated for 5 mins followed by stimulation with VEGF for 5 mins by immunoblotting analysis, IC50 = 0.1 μM. | 27326339 | ||
| NCI-H520 | Antiproliferative assay | 7 days | Antiproliferative activity against human FGFR1-amplified NCI-H520 cells after 7 days by SRB assay, IC50 = 0.281 μM. | 28521156 | ||
| HUVEC | Function assay | 10 nM | 14 hrs | Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 10 nM after 14 hrs | 16474387 | |
| HUVEC | Function assay | 100 nM | 14 hrs | Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 100 nM after 14 hrs | 16474387 | |
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
Chemische informatie, opslag en stabiliteit
| Molecuulgewicht | 523.67 | Formule | C28H41N7O3 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 219580-11-7 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | N/A | Smiles | CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C | ||
Oplosbaarheid
|
In vitro |
DMSO
: 105 mg/mL
(200.5 mM)
Ethanol : 105 mg/mL Water : 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 |
FGFR1
(Cell-free assay) ~25 nM
VEGFR2
(Cell-free assay) 100 nM-200 nM
|
|---|---|
| In vitro |
PD173074 is een ATP-competitieve remmer van FGFR1 met een Ki van ~40 nM. Deze verbinding is ook een effectieve remmer van VEGFR2. Vergeleken met FGFR1 remt het de activiteiten van Src, InsR, EGFR, PDGFR, MEK en PKC zwak met 1000-voudige of grotere IC50-waarden. Deze remmer remt autofosforylering van FGFR1 en VEGFR2 op een dosisafhankelijke manier met IC50 van respectievelijk 1-5 nM en 100-200 nM. Het remt FGF-2-bevordering van de overleving van korrelneuronen op een dosisafhankelijke manier met IC50 van 12 nM, wat een 1.000-voudig grotere potentie vertoont dan die van SU 5402. Deze chemische stof remt specifiek FGF-2-gemedieerde effecten op proliferatie, differentiatie en MAPK-activering in oligodendrocyt (OL) lijncellen. Het is actief tegen de WT-receptor en FGFR3-mutaties in multipel myeloom (MM) cellijnen. Deze verbinding remt ook potent de autofosforylering van FGFR3 op een dosisafhankelijke manier met IC50 van ~5 nM. De behandeling vermindert potent de levensvatbaarheid van FGFR3-expresserende KMS11- en KMS18-cellen met IC50 van <20 nM. Remming van aFGF-gestimuleerde MM-celgroei door dit middel correleert sterk met de expressie van FGFR3. De behandeling elimineert volledig NIH 3T3-transformatie gemedieerd door Y373C FGFR3 maar niet door Ras V12, wat aantoont dat het specifiek gericht is op FGFR3-gemedieerde celtransformatie en geen niet-specifiek cytotoxisch effect heeft. Deze chemische stof induceert ook functionele rijping van KMS11- en KMS18-cellen.
|
| Kinase Assay |
In vitro kinase remmingsassays
|
|
Assays met de full-length FGFR-1 kinase worden uitgevoerd in een totaal volume van 100 μL dat 25 mM HEPES-buffer (pH 7,4), 150 mM NaCl, 10 mM MnCl2, 0,2 mM natriumorthovanadaat, 750 μg/mL concentratie van een willekeurig copolymeer van glutaminezuur en tyrosine (4:1), verschillende concentraties PD173074 en 60 tot 75 ng enzym bevat. De reactie wordt geïnitieerd door toevoeging van [γ-32P]ATP (5 μM ATP bevattende 0,4 μCi [γ-32P]ATP per incubatie), en monsters worden geïncubeerd bij 25°C gedurende 10 minuten. De reactie wordt beëindigd door toevoeging van 30% trichloorazijnzuur en de precipitatie van materiaal op glasvezelfiltermatten. Filters worden driemaal gewassen met 15% trichloorazijnzuur, en de incorporatie van [32P] in het glutamaat-tyrosinepolymeersubstraat wordt bepaald door de radioactiviteit die op de filters achterblijft te tellen in een Wallac 1250 betaplatelezer. Niet-specifieke activiteit wordt gedefinieerd als radioactiviteit die op de filters achterblijft na incubatie van monsters zonder enzym. Specifieke activiteit wordt bepaald als totale activiteit (enzym plus buffer) min niet-specifieke activiteit. De concentratie van deze verbinding die de enzymatische activiteit van FGFR-1 met 50% remt (IC50) wordt grafisch bepaald.
|
|
| In vivo |
Toediening van PD173074 in een dosis van 1 mg/kg/dag of 2 mg/kg/dag bij muizen kan Angiogenesis, geïnduceerd door FGF of VEGF, op een dosisafhankelijke manier effectief blokkeren zonder duidelijke toxiciteit. Deze verbinding remt de in vivo groei van gemuteerde FGFR3-getransfecteerde NIH 3T3-cellen bij naakte muizen. Remming van FGFR3 door deze chemische stof vertraagt tumorgroei en verhoogt de overleving van muizen in een KMS11 xenograft myeloommodel. In de H-510 xenograft blokkeert orale toediening van deze verbinding tumorgroei op een vergelijkbare manier als bij toediening van cisplatine als enig middel, waardoor de mediane overleving toeneemt in vergelijking met controledieren die schijnbehandeling kregen. In H-69 xenografts induceert deze chemische stof complete responsen die langer dan 6 maanden aanhouden bij 50% van de muizen. Deze effecten correleren met verhoogde apoptosis in geëxcideerde tumoren, maar zijn geen gevolg van een verstoorde tumorvasculatuur.
|
Referenties |
|
Toepassingen
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | pFGFR2 / FGFR2 p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1 |
|
24968263 |
| Growth inhibition assay | Cell viability |
|
24968263 |
Technische ondersteuning
Tel: +1-832-582-8158 Ext:3
Als u nog andere vragen heeft, laat dan een bericht achter.
Veelgestelde vragen
Vraag 1:
What is the half-life of this compound (S1264) in vivo?
Antwoord:
According to literature research, it is given twice daily because this compound has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.
Producten zijn uitsluitend voor onderzoeksdoeleinden. Niet voor menselijk gebruik. Wij verkopen niet aan patiënten.
©Copyright 2013 Selleck Chemicals. Alle rechten voorbehouden.