S49076 (C007B-272657)

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.

Specifications and Purity: ≥97%

Molecular Formula: C22H22N4O4S

Molecular Weight: 438.5

PubChem CID: 49870909

Isomeric SMILES: C1COCCN1CC2=CNC(=C2)/C=C/3/C4=C(C=CC(=C4)CN5C(=O)CSC5=O)NC3=O

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