化合物AMG-208 T6260

Product Introduction
Bioactivity


英文名: AMG-208

描述: AMG-208 是一种选择性的、口服有活性的c-Met/RON 双抑制剂，对c-Met 的IC50为 9 nM。他也是CYP3A4抑制剂(IC50:32 μM)。它具有抗癌作用。

体外活性: 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. [1] Incubation of AMG-208 with rat and human liver microsomes in the presence of NADPH qualitatively yields C6-phenylarene oxidation products as the major metabolites. [1] 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. [2] AMG-208 is identified to be a c-MET and RON dual selective inhibitor. [3]

体内活性: 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, while AMG-208 (2 mg/kg i.v.) shows a bioavailability with AUC0→∞ of 2517 ng·h/mL and F of 43%, respectively. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 7.8 mg/mL (20.34 mM)


关键字: inhibit | CYPs | AMG-208 | Cytochrome P450 | c-Met/HGFR | Inhibitor | AMG208

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