产品描述
| 溶解性 |
|
| 存贮条件 | 储存温度-20°C |
| 应用 | A highly selective Met inhibitor (IC50 = 9.3 nM) |
| 产品介绍 | AMG-208是c-Met抑制剂，IC50为9.3 nM。 |
| 备注 | AMG 208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1. |
| 生化机理 | AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM . Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation . AMG-208 is identified to be a c-MET and RON dual selective inhibitor |
| 别名 | AMG208; AMG 208; 7-甲氧基-4-((6-苯基-1,2,4-三唑并(4,3-b)哒嗪-3-基)甲氧基)喹啉;;AMG208; AMG 208;7-methoxy-4-((6-phenyl-1,2,4-triazolo(4,3-b)pyridazin-3-yl)methoxy)quinoline |
