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Description: AMG 232 is a novel, potent, selective and orally bioavailable piperidinone inhibitor of MDM2-p53 protein-protein interaction with IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM. AMG 232 is currently being evaluated in human clinical trials for the treatment of cancer. p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials for multiple tumor indications.
References: J Med Chem. 2014 Aug 14; 57(15):6332-41.; Mol Cancer Ther. 2015 Mar; 14(3):649-58.; Xenobiotica. 2015; 45(8):681-92.
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