Glumetinib is a potent inhibitor of c-Met (IC50 = 0.42 nM).1 It is greater than 2,400-fold selective for c-Met over a panel of 312 kinases. Glumetinib (0.001-1 μM) inhibits c-Met phosphorylation in and proliferation of MET-overexpressing EBC-1 lung and MKN45 gastric cancer cells. It inhibits NCI H441 cell motility and invasion induced by hepatocyte growth factor (HGF) when used at a concentration of 10 nM. Glumetinib (2.5-10 mg/kg) reduces tumor volume in MKN45, SNU-5, and EBC-1 mouse xenograft models. It also reduces tumor growth in MET amplification-containing non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC) patient-derived xenograft (PDX) mouse models.WARNING This product is not for human or veterinary use.
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