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S49076

Catalog No. T3274   CAS 1265965-22-7

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.

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S49076 Chemical Structure
S49076, CAS 1265965-22-7
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
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Purity: 97.4%
Purity: 91.88%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 81 mg/mL (184.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Burbridge MF, et al. Mol Cancer Ther. 2013, 12(9):1749-62.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Reprogramming Compound Library Angiogenesis related Compound Library Cytokine Inhibitor Library Anti-Cancer Compound Library ReFRAME Related Library

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Keywords

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

 

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