AMG-208 is an orally activec-Met/RONdual selective inhibitor with anIC₅₀of 9 nM for c-Met. AMG-208 is aCYP3A4inhibitor with anIC₅₀of 32 μM. AMG-208 has anti-cancer activity^[1][2][3].

AMG-208 (compound 4) treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC₅₀of 46 nM^[1].
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 IC₅₀of 4.1 μM, which is an eightfold decrease relative to the IC₅₀(32 μM) without preincubation^[2].

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^[1].

383.40

Solid

C₂₂H₁₇N₅O₂

1002304-34-8

Room temperature in continental US; may vary elsewhere.

DMSO : 3.33 mg/mL(8.69 mM;Need ultrasonic)

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