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Description: Savolitinib (other names used: volitinib, AZD6094, HMPL-504) is a novel, potent, orally active and selective inhibitor of the c-Met receptor kinase. It is currently in clinical trials for various indications such as PRCC. Savolitinib has IC50 values of 5 nM and 3 nM for c-Met and p-Met respectively. It exhibits high selectivity for c-Met over 274 other kinases. Savolitinib selectively binds to the ATP-site and inhibits the activation of c-Met, eventually disrupts transduction of c-Met signal pathways, collectively this will result in cell growth inhibition in tumors overexpressing the c-Met protein, as a result, Savolitinib has potential anticancer activity.
References: Mol Oncol. 2015 Jan; 9(1):323-33; J Med Chem. 2014 Sep 25; 57(18):7577-89.
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