Powder: -20°C for 3 years | In solvent: -80°C for 1 year
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 39.00 | |
2 mg | In stock | $ 57.00 | |
5 mg | In stock | $ 76.00 | |
10 mg | In stock | $ 97.00 | |
25 mg | In stock | $ 179.00 | |
50 mg | In stock | $ 322.00 | |
100 mg | In stock | $ 588.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 84.00 |
Description | S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs. |
Targets&IC50 | Axl:7 nM, Mer:2 nM, FGFR2:17 nM, Met:1 nM, FGFR3:15 nM |
In vitro | S49076 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[1]. |
In vivo | S49076 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[1]. |
Cell Research | For GTL-16 and SNU-16 viability assays, cells are seeded in 96-well microplates at the appropriate density in media containing 10% FCS and supplemented 48 hours later with serial dilutions of S49076 in a final volume of 150 μL per well. After 96 hours (GTL-16) or 120 hours (SNU-16) incubation, 15 μL of a solution of 5 mg/mL MTT is added to each well and the plates are incubated for 4 hours at 37℃. The formazan metabolite is solubilized in SDS for SNU-16 and, following removal of the MTT solution, in DMSO for GTL-16. Global cell viability is estimated by measurement of optical density at 540 nm. (Only for Reference) |
Molecular Weight | 438.5 |
Formula | C22H22N4O4S |
CAS No. | 1265965-22-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 81 mg/mL (184.9 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
S49076 1265965-22-7 Angiogenesis Tyrosine Kinase/Adaptors TAM Receptor c-Met/HGFR FGFR Fibroblast growth factor receptor inhibit Inhibitor S 49076 S-49076 inhibitor