réservé à la recherche
Axitinib (AG-013736) Inhibiteur de la Tyrosine Kinase
N° Cat.S1005
Structure chimique
Poids moléculaire: 386.47
Aller à
Contrôle qualité
Lot :
Pureté :
99.96%
99.96
| Cibles apparentées | EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit |
|---|---|
| Autre VEGFR Inhibiteurs | SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | ||
| Cliquez pour voir plus de données expérimentales sur les lignées cellulaires | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 386.47 | Formule | C22H18N4OS |
Stockage (À partir de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 319460-85-0 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | AG 013736 | Smiles | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4 | ||
Solubilité
|
In vitro |
DMSO
: 26 mg/mL
(67.27 mM)
Water : Insoluble Ethanol : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.
Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Fonctionnalités |
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 pourrait bloquer l'autophosphorylation cellulaire du VEGFR et la viabilité des cellules endothéliales médiée par le VEGF, la formation de tubes et la signalisation en aval. Ce composé inhibe la prolifération de lignées cellulaires variables avec des IC50 de >10 000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) et 573 nM (HUVEC non stimulées par le VEGF).
|
| Kinase Assay |
Test de phosphorylation de la kinase du récepteur cellulaire
|
|
Des cellules endothéliales de l'aorte porcine (PAE), qui surexpriment les VEGFR2, PDGFR
D
, Kit pleine longueur, et des NIH-3T3, qui surexpriment le VEGFR2 murin (Flk-1) ou le PDGFR
D
, sont générées. Les plaques à 96 puits sont recouvertes de 100
D
L/puits de 2,5
D
g/mL d'anticorps anti-VEGFR2, 0,75
D
g/mL d'anticorps anti-PDGFR
D
, 0,25
D
g/mL d'anticorps anti-PDGFR
D
, 0,5
D
g/mL d'anticorps anti-KIT, ou 1,20
D
g/mL d'anticorps anti-Flk-1 pour préparer les plaques de capture ELISA. La phosphorylation de la RTK est ensuite mesurée par ELISA.
|
|
| In vivo |
Axitinib présente une inhibition primaire sur des modèles transplantés orthotopiquement tels que M24met (mélanome), HCT-116 (cancer colorectal) et SN12C (carcinome rénal). Ce composé retarde la croissance tumorale de 11,4 jours par rapport aux contrôles (p.o. 30 mg/kg) et diminue la densité moyenne des vaisseaux (MVD) à 21, contre 49 chez les contrôles, dans les xénogreffes de flanc IGR-N91. Il inhibe significativement la croissance et perturbe la microvasculature tumorale dans le modèle de cancer du sein BT474 à 10-100 mg/kg. Il a montré une activité en monothérapie dans diverses tumeurs, y compris le carcinome rénal, le cancer de la thyroïde, le cancer du poumon non à petites cellules et le mélanome.
|
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | 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 | Cell viability |
|
26474283 |
Informations sur lessai clinique
(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Sponsor/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT06161558 | Not yet recruiting | Neoplasms |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
May 15 2024 | Phase 1 |
| NCT05949632 | Recruiting | Advanced Solid Tumors |
Incyte Corporation |
April 16 2024 | Phase 1|Phase 2 |
| NCT05969496 | Recruiting | Renal Cancer|Kidney Cancer|Renal Cell Carcinoma|Inferior Vena Cava Thrombosis |
University of Colorado Denver|Cancer League of Colorado |
December 4 2023 | Phase 2 |
| NCT05904730 | Enrolling by invitation | Breast Cancer|Ovarian Cancer|Breast Neoplasms|Ovarian Neoplasms|BRCA Mutation|HER2-positive Breast Cancer|HER2-negative Breast Cancer|HER-2 Protein Overexpression |
Lynkcell Europe |
July 11 2023 | Phase 1 |
| NCT05817903 | Recruiting | Metastatic Renal Cell Carcinoma |
Consorzio Oncotech|Pfizer |
April 18 2023 | Phase 2 |
| NCT05263609 | Withdrawn | Renal Cell Cancer |
University of Oklahoma|Merck Sharp & Dohme LLC|Pfizer |
June 2022 | Phase 2 |
Support technique
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Questions fréquemment posées
Question 1:
We would like to store it at -80℃ after this compound is dissolved in CMC. Do you have any information about the suggested concentration in CMC?
Réponse :
In 0.5% CMC at up to 30mg/ml, it is a suspension for oral gavage administration only. We don't suggest customer to freeze down the solution but to make fresh if possible. Customer can store it for 1-2 weeks at 4 degree for continuous use.
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