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AMG-208

CAS No. : 1002304-34-8

MCE 国际站：AMG-208

产品活性：AMG-208 是一种口服有效的，选择性 c-Met/RON 双抑制剂，对 c-Met 的 IC₅₀ 为 9 nM。AMG-208 是一种 CYP3A4 抑制剂，IC₅₀ 为 32 μM。AMG-208 具有抗癌活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Metabolic Enzyme/Protease

作用靶点：c-Met/HGFR  |  Cytochrome P450

In Vitro: AMG-208 (compound 4) 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 (compound 1) 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.

In Vivo: In male Sprague Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour.

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