| 产品描述： | FGFR1 选择性抑制剂;FGFR1 Selective Inhibitors;;InformationS49076 is a novel, potent inhibitor ofMet (c-Met),AXL/MER, andFGFR1/2/3with IC50 values below 20 nmol/L.TargetsMet (Cell-free assay); Mer (Cell-free assay); Axl (Cell-free assay); FGFR3 (Cell-free assay); FGFR2 (Cell-free assay) 16457,1 nM; 2 nM; 7 nM; 15 nM; 17 nMIn vitroS49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling in vitro and in vivo. In cell models, S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. S49076 inhibits viability, motility, and three-dimensional colony formation of cancer cells expressing MET, AXL, or FGFRs.In vivoS49076 shows marked antitumor activity in MET- and FGFR-dependent tumor xenografts at well-tolerated doses. S49076 has high distribution to tumors, in which the half-life for the dose of 3.125 mg/kg is approximately 7 hours versus less than 2 hours in the blood. At doses of 6.25 mg/kg and higher, more than 50% inhibition of MET phosphorylation is retained at 16 hours. S49076 is also active in a bevacizumab-resistant model and totally inhibits the growth of colon carcinoma xenografts in association with bevacizumab.Cell Research(from reference)Cell lines：GTL-16 and SNU-16 cell lines Incubation Time：96 h or 120 h |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京