| 应用 |
An ATP-competitive inhibitor against VEGFR-2, Flk-1, VEGFR-1 and FGFR-1 |
| 产品介绍 |
Brivanib (BMS-540215)是一种ATP竞争性的VEGFR2抑制剂，IC50为25 nM，对VEGFR-1和FGFR-1抑制作用适中，但比作用于PDGFR-β效果强240多倍。 |
| 备注 |
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3. |
| 生化机理 |
Brivanib is an ATP-competitive inhibitor against human VEGFR-2 and mouse Flk-1 with IC50 of 25 nM and 89 nM, respectively. Brivanib also inhibits VEGFR-1 and FGFR-1 with IC50 of 0.38 and 0.148 μM. Brivanib displays antitumor activities in H3396 xenograft. This compound completely inhibits the tumor growth, with TGI of 85% and 97%, respectively. |
| 别名 |
1-[[4-[(4-氟-2-甲基-1H-吲哚-5-基)氧基]-5-甲基吡咯并[2,1-f][1,2,4]三嗪-6-基]氧基]-2-丙醇; 酪氨酸激酶抑制剂;BMS-540215; BMS540215; BMS 540215;(2R)-1-[4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4 ]triazin-6-yloxy]propanol |
