[CAS NO. 1265965-22-7] S49076
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PRODUCTS SPECIFICATIONS [1265965-22-7]
Catalog
SLK-S8404
Brand
Selleck
CAS
1265965-22-7
DESCRIPTION [1265965-22-7]
Overview
| MDL | MFCD28963943 |
|---|---|
| Molecular Weight | 438.50 |
| Molecular Formula | C22H22N4O4S |
| SMILES | O=C(N1CC2=CC3=C(NC(/C3=C\C4=CC(CN5CCOCC5)=CN4)=O)C=C2)SCC1=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
S49076 is a novel, potent inhibitor of , , and with IC50 values below 20 nmol/L.
Targets
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.
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.
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