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Savolitinib is an inhibitor of c-Met (IC50 = 5 nM).1 It is selective for c-Met over a panel of 274 other kinases at 1 µM. Savolitinib inhibits c-Met autophosphorylation in NCI H441 human non-small cell lung cancer (NSCLC) cells (IC50 = 3 nM). It also inhibits proliferation of NCI H441 cells induced by HGF (Item No. 32052; IC50 = 6 nM) and in a panel of gastric cancer cells with dysregulated c-Met (EC50s = 0.6-14.7 nM).1,2 Savolitinib (3 mg/kg) inhibits intratumor c-Met autophosphorylation by 94% and reduces tumor growth in an Hs 746T human stomach cancer mouse xenograft model.2
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1. Discovery of (S)-
2. Volitinib, a potent and highly selective c-