solo per uso di ricerca
N. Cat.S1005
| Target correlati | EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit |
|---|---|
| Altro VEGFR Inibitori | SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | PMID |
|---|---|---|---|---|---|---|
| EoL-1-cell | Growth Inhibition Assay | IC50=0.0000513 μM | SANGER | |||
| NCI-H1703 | Growth Inhibition Assay | IC50=0.000902 μM | SANGER | |||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.00682 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.00722 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=0.00992 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.10836 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=0.11005 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.16577 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.16816 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.17665 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=0.23989 μM | SANGER | |||
| G-361 | Growth Inhibition Assay | IC50=0.32325 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=0.37642 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.3932 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=0.42127 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.42361 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=0.44776 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=0.51008 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=0.72113 μM | SANGER | |||
| SW756 | Growth Inhibition Assay | IC50=0.99846 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=1.01146 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=1.01801 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=1.06422 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=1.06633 μM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=1.08389 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=1.10381 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=1.11334 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=1.11395 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=1.14694 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=1.17248 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=1.25457 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=1.32557 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=1.39042 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=1.40683 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=1.43996 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=1.56909 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=1.60556 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=1.65158 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=1.66383 μM | SANGER | |||
| HMV-II | Growth Inhibition Assay | IC50=1.70488 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=1.80015 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=1.82163 μM | SANGER | |||
| PA-1 | Growth Inhibition Assay | IC50=1.82725 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=1.86281 μM | SANGER | |||
| HSC-4 | Growth Inhibition Assay | IC50=1.93839 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=2.00916 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=2.13424 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=2.13606 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=2.20598 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=2.21671 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=2.23834 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=2.23875 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=2.24957 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=2.28061 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=2.42165 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=2.47168 μM | SANGER | |||
| T-24 | Growth Inhibition Assay | IC50=2.48037 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=2.53013 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=2.59169 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=2.66345 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=2.70299 μM | SANGER | |||
| CHP-212 | Growth Inhibition Assay | IC50=2.82091 μM | SANGER | |||
| DMS-273 | Growth Inhibition Assay | IC50=2.90207 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=3.02597 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=3.15005 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=3.22805 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=3.27657 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=3.30017 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=3.33875 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=3.34999 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=3.50396 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=3.62616 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=3.63022 μM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=3.63334 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=3.83094 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=3.91808 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=3.93911 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=3.99126 μM | SANGER | |||
| HCC1395 | Growth Inhibition Assay | IC50=3.99484 μM | SANGER | |||
| DU-145 | Growth Inhibition Assay | IC50=4.12825 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=4.15916 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=4.21597 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=4.22177 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=4.24192 μM | SANGER | |||
| CAL-27 | Growth Inhibition Assay | IC50=4.24344 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=4.26658 μM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=4.2966 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=4.31468 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=4.53014 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=4.55163 μM | SANGER | |||
| SNU-423 | Growth Inhibition Assay | IC50=4.6079 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=4.6977 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=4.81418 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=4.89048 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=4.97352 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=4.99908 μM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=5.03514 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=5.29827 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=5.38185 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=5.41737 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=5.57849 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=5.72325 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=5.75583 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=5.84325 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=5.87918 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=5.91504 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=5.92395 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=5.92771 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=5.98821 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=6.10574 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=6.10599 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=6.11248 μM | SANGER | |||
| MKN45 | Growth Inhibition Assay | IC50=6.26016 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=6.28857 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=6.41688 μM | SANGER | |||
| S-117 | Growth Inhibition Assay | IC50=6.50267 μM | SANGER | |||
| HCC1569 | Growth Inhibition Assay | IC50=6.53737 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=6.54572 μM | SANGER | |||
| OC-314 | Growth Inhibition Assay | IC50=6.91159 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=7.01072 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=7.19345 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=7.2072 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=7.32386 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=7.4815 μM | SANGER | |||
| HCC1419 | Growth Inhibition Assay | IC50=7.53 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=7.60644 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=7.60743 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=7.63033 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=7.64934 μM | SANGER | |||
| SW1088 | Growth Inhibition Assay | IC50=7.65826 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=7.68613 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=7.6961 μM | SANGER | |||
| MDA-MB-415 | Growth Inhibition Assay | IC50=7.89186 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=7.94492 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=8.15783 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=8.2172 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=8.44316 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=8.51534 μM | SANGER | |||
| 8505C | Growth Inhibition Assay | IC50=8.64824 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=8.78439 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=8.99551 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=9.01433 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition Assay | IC50=9.02241 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=9.1887 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=9.41944 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=9.45234 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=9.60237 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=9.63072 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=9.83384 μM | SANGER | |||
| MEL-JUSO | Growth Inhibition Assay | IC50=9.90127 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=9.90203 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=9.90909 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=10.0665 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=10.1045 μM | SANGER | |||
| T47D | Growth Inhibition Assay | IC50=10.155 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=10.3533 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=10.4402 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=10.4432 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=10.4718 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=10.6301 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=10.6361 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=10.7068 μM | SANGER | |||
| HuP-T4 | Growth Inhibition Assay | IC50=11.0328 μM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=11.2657 μM | SANGER | |||
| HO-1-N-1 | Growth Inhibition Assay | IC50=11.3398 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=11.5378 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=11.5985 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=11.7248 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=11.8581 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=11.9064 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=11.932 μM | SANGER | |||
| 23132-87 | Growth Inhibition Assay | IC50=12.0821 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=12.3285 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=12.5026 μM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=12.5577 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=12.765 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=12.8258 μM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=12.9276 μM | SANGER | |||
| PFSK-1 | Growth Inhibition Assay | IC50=12.9507 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=13.0779 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=13.3641 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=13.4541 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition Assay | IC50=13.5136 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=13.5349 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=13.5887 μM | SANGER | |||
| SiHa | Growth Inhibition Assay | IC50=13.8346 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=13.8808 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=13.9928 μM | SANGER | |||
| HT-1197 | Growth Inhibition Assay | IC50=14.0809 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=14.1362 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=14.5774 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=14.627 μM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=14.7888 μM | SANGER | |||
| SKG-IIIa | Growth Inhibition Assay | IC50=14.8001 μM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=14.9933 μM | SANGER | |||
| NCI-H2029 | Growth Inhibition Assay | IC50=15.3602 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=15.5095 μM | SANGER | |||
| LK-2 | Growth Inhibition Assay | IC50=15.6449 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=15.9075 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=16.0676 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=16.342 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=16.4485 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=16.565 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=16.6971 μM | SANGER | |||
| NCI-H460 | Growth Inhibition Assay | IC50=16.7326 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=16.7877 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=16.8111 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=16.8625 μM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=16.9488 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition Assay | IC50=17.1908 μM | SANGER | |||
| AU565 | Growth Inhibition Assay | IC50=17.225 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=17.5317 μM | SANGER | |||
| 22RV1 | Growth Inhibition Assay | IC50=17.5884 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=17.6598 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=17.7031 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=17.7184 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=17.8489 μM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=17.9249 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=17.9635 μM | SANGER | |||
| COR-L23 | Growth Inhibition Assay | IC50=18.0011 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=18.2276 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=18.4615 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=18.5697 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=18.5883 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=18.6502 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=19.0592 μM | SANGER | |||
| EPLC-272H | Growth Inhibition Assay | IC50=19.3708 μM | SANGER | |||
| SW948 | Growth Inhibition Assay | IC50=19.3934 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=19.4546 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=20.2141 μM | SANGER | |||
| CP50-MEL-B | Growth Inhibition Assay | IC50=20.4748 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=20.4978 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=20.7967 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=20.906 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=20.9285 μM | SANGER | |||
| NB12 | Growth Inhibition Assay | IC50=21.0394 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=21.582 μM | SANGER | |||
| PSN1 | Growth Inhibition Assay | IC50=21.6453 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=21.7454 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=22.3031 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=22.3498 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=22.4752 μM | SANGER | |||
| D-542MG | Growth Inhibition Assay | IC50=22.5558 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=22.6439 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=22.8368 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=23.1478 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=23.1944 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition Assay | IC50=23.4681 μM | SANGER | |||
| NCI-H520 | Growth Inhibition Assay | IC50=23.4948 μM | SANGER | |||
| ESS-1 | Growth Inhibition Assay | IC50=23.8059 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=23.9475 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=24.0312 μM | SANGER | |||
| HCC1937 | Growth Inhibition Assay | IC50=24.1 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=24.142 μM | SANGER | |||
| HCC38 | Growth Inhibition Assay | IC50=24.2394 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=24.6162 μM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=24.6258 μM | SANGER | |||
| YAPC | Growth Inhibition Assay | IC50=24.8214 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=25.2611 μM | SANGER | |||
| SK-N-AS | Growth Inhibition Assay | IC50=25.8584 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=26.049 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=26.2038 μM | SANGER | |||
| NCI-H810 | Growth Inhibition Assay | IC50=26.3112 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=26.5454 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=26.5529 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=26.7382 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=26.8018 μM | SANGER | |||
| NCI-H2052 | Growth Inhibition Assay | IC50=27.086 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=27.2102 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=27.7767 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=27.8005 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=27.8532 μM | SANGER | |||
| PC-3 | Growth Inhibition Assay | IC50=27.8941 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=27.9343 μM | SANGER | |||
| U-118-MG | Growth Inhibition Assay | IC50=28.0123 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=28.0822 μM | SANGER | |||
| CAMA-1 | Growth Inhibition Assay | IC50=28.8564 μM | SANGER | |||
| MC-IXC | Growth Inhibition Assay | IC50=29.2366 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=29.3172 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=29.321 μM | SANGER | |||
| KP-4 | Growth Inhibition Assay | IC50=29.516 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=29.5445 μM | SANGER | |||
| 5637 | Growth Inhibition Assay | IC50=29.6421 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=29.7269 μM | SANGER | |||
| Ca-Ski | Growth Inhibition Assay | IC50=29.946 μM | SANGER | |||
| AsPC-1 | Growth Inhibition Assay | IC50=30.0212 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=30.15 μM | SANGER | |||
| L-428 | Growth Inhibition Assay | IC50=30.405 μM | SANGER | |||
| SW1463 | Growth Inhibition Assay | IC50=30.5383 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=30.5574 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=30.7702 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=31.0263 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=31.1164 μM | SANGER | |||
| A375 | Growth Inhibition Assay | IC50=31.1696 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=31.2435 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition Assay | IC50=31.4271 μM | SANGER | |||
| ME-180 | Growth Inhibition Assay | IC50=31.6542 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=31.8247 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=32.1446 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=32.1971 μM | SANGER | |||
| SNU-387 | Growth Inhibition Assay | IC50=32.3191 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=32.3353 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=32.9408 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=33.5136 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=33.5621 μM | SANGER | |||
| LU-135 | Growth Inhibition Assay | IC50=33.801 μM | SANGER | |||
| NCI-H2122 | Growth Inhibition Assay | IC50=33.9966 μM | SANGER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=34.4107 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=34.8515 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=35.2747 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=35.3038 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=35.5042 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=35.6545 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=36.0496 μM | SANGER | |||
| EW-22 | Growth Inhibition Assay | IC50=36.4072 μM | SANGER | |||
| IGR-1 | Growth Inhibition Assay | IC50=36.8184 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=37.125 μM | SANGER | |||
| M14 | Growth Inhibition Assay | IC50=37.1642 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=37.2794 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=37.4501 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=37.9412 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=37.9582 μM | SANGER | |||
| SW620 | Growth Inhibition Assay | IC50=38.4974 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=39.8205 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=40.1268 μM | SANGER | |||
| HN | Growth Inhibition Assay | IC50=40.1782 μM | SANGER | |||
| HCT-15 | Growth Inhibition Assay | IC50=40.5907 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=40.9157 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=41.3015 μM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=41.4725 μM | SANGER | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=41.7767 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=41.9821 μM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=42.2699 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=42.8958 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition Assay | IC50=43.4944 μM | SANGER | |||
| CAL-51 | Growth Inhibition Assay | IC50=43.5605 μM | SANGER | |||
| RH-18 | Growth Inhibition Assay | IC50=43.805 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=43.8347 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=44.009 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=45.2621 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=45.7365 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=46.111 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=46.5533 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=46.8117 μM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=46.9805 μM | SANGER | |||
| U251 | Growth Inhibition Assay | IC50=46.994 μM | SANGER | |||
| MKN1 | Growth Inhibition Assay | IC50=47.5137 μM | SANGER | |||
| A431 | Growth Inhibition Assay | IC50=47.8338 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=49.2039 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=49.4064 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=49.4444 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=49.6075 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=49.9332 μM | SANGER | |||
| MCF7 | Antiproliferative assay | 5 days | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 0.97 μM. | 23829549 | ||
| MDA-MB-468 | Antiproliferative assay | 5 days | Antiproliferative activity against human MDA-MB-468 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 1.3 μM. | 23829549 | ||
| HCC1954 | Antiproliferative assay | 5 days | Antiproliferative activity against human HCC1954 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 2.7 μM. | 23829549 | ||
| SKBR3 | Antiproliferative assay | 5 days | Antiproliferative activity against human SKBR3 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 3.8 μM. | 23829549 | ||
| MDA-MB-231 | Antiproliferative assay | 5 days | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by SRB assay, GI50 = 7.3 μM. | 23829549 | ||
| MCF7 | Cytotoxicity assay | 5 days | Cytotoxicity against human MCF7 cells after 5 days by SRB assay, GI50 = 2.3 μM. | 24867403 | ||
| MDA-MB-468 | Cytotoxicity assay | 5 days | Cytotoxicity against human MDA-MB-468 cells after 5 days by SRB assay, GI50 = 2.8 μM. | 24867403 | ||
| SKBR3 | Cytotoxicity assay | 5 days | Cytotoxicity against human SKBR3 cells after 5 days by SRB assay, GI50 = 4.6 μM. | 24867403 | ||
| MDA-MB-231 | Cytotoxicity assay | 5 days | Cytotoxicity against human MDA-MB-231 cells after 5 days by SRB assay, GI50 = 11 μM. | 24867403 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| HUVEC | Antiproliferative assay | 1 hr | Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs by MTT assay, IC50 = 0.0005 μM. | ChEMBL | ||
| HUVEC | Antiproliferative assay | 1 hr | Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as reduction in cell viability preincubated for 1 hr followed by addition of VEGF measured after 72 hrs in presence of albumin by MTT assay, IC50 = 0.0027 μM. | ChEMBL | ||
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against VEGF-stimulated human A549 cells after 48 hrs by CCK8 assay, IC50 = 22.4 μM. | ChEMBL | ||
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against VEGF-stimulated human HepG2 cells after 48 hrs by CCK8 assay, IC50 = 38.7 μM. | ChEMBL | ||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 386.47 | Formula | C22H18N4OS |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 319460-85-0 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | AG 013736 | Smiles | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4 | ||
|
In vitro |
DMSO
: 26 mg/mL
(67.27 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
| Caratteristiche |
Superior as second-line therapy relative to sorafenib (current standard-of-care).
|
|---|---|
| Targets/IC50/Ki |
VEGFR1/FLT1
(Porcine aorta endothelial cells) 0.1 nM
VEGFR2/Flk1
(Porcine aorta endothelial cells) 0.18 nM
VEGFR2/KDR
(Porcine aorta endothelial cells) 0.2 nM
VEGFR3
(Porcine aorta endothelial cells) 0.1 nM-0.3 nM
PDGFRβ
(Porcine aorta endothelial cells) 1.6 nM
Kit
(Porcine aorta endothelial cells) 1.7 nM
PDGFRα
(Porcine aorta endothelial cells) 5.0 nM
|
| In vitro |
Axitinib potrebbe bloccare l'autofosforilazione cellulare del VEGFR e la vitalità delle cellule endoteliali mediata dal VEGF, la formazione di tubi e la segnalazione a valle. Questo composto inibisce la proliferazione di diverse linee cellulari con IC50 di >10.000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) e 573 nM (HUVEC non stimolate dal VEGF).
|
| Saggio chinasico |
Saggio di fosforilazione della chinasi del recettore cellulare
|
|
Vengono generate cellule endoteliali dell'aorta suina (PAE), che sovraesprimono VEGFR2, PDGFRβ, Kit a lunghezza intera, e NIH-3T3, che sovraesprimono VEGFR2 murino (Flk-1) o PDGFRα. Le piastre a 96 pozzetti vengono rivestite con 100 μL/pozzetto di 2.5 μg/mL di anticorpo anti-VEGFR2, 0.75 μg/mL di anticorpo anti-PDGFRβ, 0.25 μg/mL di anticorpo anti-PDGFRα, 0.5 μg/mL di anticorpo anti-KIT o 1.20 μg/mL di anticorpo anti-Flk-1 per preparare le piastre di cattura ELISA. La fosforilazione della RTK viene quindi misurata mediante ELISA.
|
|
| In vivo |
Axitinib mostra un'inibizione primaria nei modelli trapiantati ortotopicamente come M24met (melanoma), HCT-116 (cancro colorettale) e SN12C (carcinoma a cellule renali). Questo composto ritarda la crescita tumorale di 11,4 giorni rispetto ai controlli (p.o. 30 mg/kg) e diminuisce la densità media dei vasi (MVD) a 21, rispetto a 49 nei controlli, negli xenotrapianti al fianco IGR-N91. Inibisce significativamente la crescita e interrompe la microvascolarizzazione tumorale nel modello di cancro al seno BT474 a 10-100 mg/kg. Ha mostrato attività come agente singolo in vari tumori, inclusi carcinoma a cellule renali, cancro alla tiroide, cancro al polmone non a piccole cellule e melanoma.
|
Riferimenti |
|
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | p-c-kit / c-kit / p-AKT / AKT / p-ERK / ERK / p-STAT3 / STAT3 / p-STAT5 / STAT5 / p-S6K / S6K / p-S6 / S6 PARP / cleaved PARP / caspase-3 / cleaved caspase-3 |
|
31205508 |
| Immunofluorescence | alpha-tubulin |
|
26474283 |
| Growth inhibition assay |