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S49076 hydrochloride

Chemical Structure : S49076 hydrochloride

CAS No.: 1265966-31-1

S49076 hydrochloride (S 49076;S-49076)

Catalog No.: PC-50012Not For Human Use, Lab Use Only.

S49076 hydrochloride is a potent, ATP-competitive tyrosine kinase inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 of <20 nM, also potently inhibits the kinase activity of mutated isoforms of MET (D1246N, Y1248D, Y1248H) and FGFR1/2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

S49076 hydrochloride is a potent, ATP-competitive tyrosine kinase inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 of <20 nM, also potently inhibits the kinase activity of mutated isoforms of MET (D1246N, Y1248D, Y1248H) and FGFR1/2; only inhibits 6% of kinases on a panel of 442 human wild-type and mutated kinases at 100 nM; 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; causes tumor growth arrest in bevacizumab-resistant tumors in cancer xenograft models.

Brain Cancer

Phase 2 Clinical

Physicochemical Properties

M.Wt 474.96
Formula C22H23ClN4O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[[2,3-dihydro-3-[[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene]-2-oxo-1H-indol-5-yl]methyl]-2,4-thiazolidinedione hydrochloride

References

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

2. Clémenson C, et al. Mol Cancer Ther. 2017 Oct;16(10):2107-2119.

3. Rodon J, et al. Eur J Cancer. 2017 Aug;81:142-150.

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