产品介绍 |
AC480 (BMS-599626)是 HER1和HER2选择性高效抑制剂,IC50分别为20 nM和30 nM,比针对VEGFR2,c-Kit,Lck,MET的抑制性强100倍以上。 |
备注 |
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1. |
生化机理 |
BMS-599626 is a potent inhbitor of human epidermal growth factor receptors 1 and 2 (HER1 and HER2, IC50 = 20 and 30 nM, respectively). BMS599626 inhibits proliferation of several HER-expressing cancer cell lines, including HER2-overexpressing breast cancer lines, but does not affect the proliferation rate of HER-negative cancer cell lines |
别名 |
[4-[[1-(3-氟苄基)-1H-吲唑-5-基]氨基]-5-甲基吡咯并[2,1-f][1,2,4]三嗪-6-基]氨基甲酸(S)-吗啉-3-基甲酯;BMS-599626;BMS599626;AC480;BMS 599626;AC-480;AC 480; (3S)-3-Morpholinylmethyl-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-Carbamic acid |