产品描述:
NPS 1034 is a dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM), receptors for hepatocyte growth factor and vitamin K-dependent proteins, respectively.{33325} It synergistically inhibits cell proliferation when used in combination with gefitinib (Item No. 13166) or erlotinib (Item No. 10483) in NSCLC cells with acquired resistance to EGFR receptor tyrosine kinase inhibitors.{33325} NPS 1034 inhibits autophosphorylation of numerous constitutively active mutant forms of MET (IC50s <25 nM) and inhibits the invasion and migration of MET mutant-transfected cells.{33326} It also inhibits growth of MKN45 xenograft tumors in mice treated orally with 30 mg/kg NPS 1034 for 25 days.{33326}