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執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.
Description: S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 was established and correlated well with impact on tumor growth. MET, AXL, and the FGFRs have all been implicated in resistance to VEGF/VEGFR inhibitors such as bevacizumab. A phase I study with S-49076 is currently underway in patients with advanced solid tumors.
Name: S-49076
CAS#: 1265965-22-7
Chemical Formula: C22H22N4O4S
Exact Mass: 438.13618
Molecular Weight: 438.502
Elemental Analysis: C, 60.26; H, 5.06; N, 12.78; O, 14.59; S, 7.31
Synonym: S-49076; S49076; S 49076.
IUPAC/Chemical Name: (Z)-3-((3-((4-(morpholinomethyl)-1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)methyl)thiazolidine-2,4-dione
InChi Key: AREYWCZYVPSHGS-NVMNQCDNSA-N
InChi Code: InChI=1S/C22H22N4O4S/c27-20-13-31-22(29)26(20)12-14-1-2-19-17(8-14)18(21(28)24-19)9-16-7-15(10-23-16)11-25-3-5-30-6-4-25/h1-2,7-10,23H,3-6,11-13H2,(H,24,28)/b18-9-
SMILES Code: O=C(N1CC2=CC3=C(NC(/C3=C\C4=CC(CN5CCOCC5)=CN4)=O)C=C2)SCC1=O
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code: 293490
ADDITIONAL INFORMATION
Related CAS#
1265965-22-7(S-49076 Free Base)
1265966-31-1(722572
REFERENCES
1: Burbridge MF, Bossard CJ, Saunier C, Fejes I, Bruno A, Léonce S, Ferry G, Da
Violante G, Bouzom F, Cattan V, Jacquet-Bescond A, Comoglio PM, Lockhart BP,
Boutin JA, Cordi A, Ortuno JC, Pierré A, Hickman JA, Cruzalegui FH, Depil S.
S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical
activity alone and in association with bevacizumab. Mol Cancer Ther. 2013
Sep;12(9):1749-62. doi: 10.1158/1535-7163.MCT-13-0075. Epub 2013 Jun 26. PubMed
PMID: 23804704.
