Unii-U2Y5ofn795

Product Name: Unii-U2Y5ofn795

Synonyms: Bms 582664;Bms582664;Brivanib alaninate;L-Alanine, (1R)-2-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo(2,1-F)(1,2,4)triazin-6-yl)oxy)-1-methylethyl ester;Unii-U2Y5ofn795;(1R)-2-((4-((4-Fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)-1-methylethyl L-alanine ester;Brivanib alaninate(BMS-582664);L-Alanine (1R)-2-[[4-[(4-fluoro-2-Methyl-1H-indol-5-yloxy)]-5-Methyl-1H-pyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]isopropyl ester

CAS: 649735-63-7

MF: C19H18FN4O3

MW: 369.3696232

Product Categories: Aromatics;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Anti-cancer & immunity

Purity : 99%

Appearance : White powders

Package : 1kg/foil bag

Usage :A novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor.

Usage BMS-582664 is an oral VEGFR/FGFR inhibitor for VEGFR2, Flk1, VEGFR1 and FGFR1 with IC50 of 25 nM, 89 nM, 380 nM and 148 nM, respectively.

Application:

[1] BMS-582664 inhibits VEGF and FGF-stimulated HUVECs proliferation, IC50 of 40 nM, respectively, and 276 nM.

[2] BMS-582664 (2 μM) acting on the VEGF and bFGF stimulated SK-HEP1 cells and HepG-2 cells, significantly inhibited VEGFR-2, FGFR-1, ERK1 / 2 and Akt phosphorylation, and BMS-582664 alone in unstimulated cells, then the ERK1 / 2, Akt, VEGFR-2, and the level of phosphorylation of FGFR-1 has no effect.

[3] BMS-582664 to inhibit CYP2C19, CYP3A4 (BFC) and CYP3A4 (BzRes), IC50 were 2.4 μM, 0.51 μM and 1.6 μM. BMS-582664 has a high solid state stability (only 0.3% in the desiccant during 12 weeks at 50 ° C degradation), while at pH 6.5 also has considerable liquid stability.

Attention:Only for research and not for human trial!

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