All Photos(1)
Synonym(s):
(2R)-1-[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-ol, (2R)-1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol, (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, BMS 540215, BMS 582664 active drug, BMS-540215, BMS-582664 active drug, BMS540215, BMS582664 active drug
Empirical Formula (Hill Notation):
C19H19FN4O3
CAS Number:
Molecular Weight:
370.38
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.25
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
Brivanib (BMS-540215) is an orally active, ATP-competitive FGF & VEGF receptor tyrosine kinase inhibitor (VEGFR-1/2/3 IC50 = 380/25/10 nM; FGFR-1/2/3 IC50 = 148/125/68 nM). Brivanib inhibits VEGF-stimulated and basic FGF-stimulated proliferation in endothelial cultures (IC50 = 40 & 276 nM, respectively) and displays antitumor efficacy in vivo (30-90 mg/kg via daily p.o. in mice with H3396 xenografts).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Rajeev S Bhide et al.
Journal of medicinal chemistry, 49(7), 2143-2146 (2006-03-31)
A series of substituted 4-(4-fluoro-1H-indol-5-yloxy)pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of vascular endothelial growth factor receptor-2 kinase is reported. Structure-activity relationship studies revealed that a methyl group at the 5-position and a substituted alkoxy group at the 6-position of the pyrrolo[2,1-f][1,2,4]triazine core gave potent
Hung Huynh et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 14(19), 6146-6153 (2008-10-03)
Hepatocellular carcinoma (HCC) is the fifth most common primary neoplasm; surgery is the only curative option but 5-year survival rates are only 25% to 50%. Vascular endothelial growth factor (VEGF) and fibroblast growth factor (FGF) are known to be involved
Punit H Marathe et al.
Cancer chemotherapy and pharmacology, 65(1), 55-66 (2009-04-28)
Brivanib alaninate is a prodrug of brivanib (BMS-540215), a potent oral VEGFR-2 inhibitor and is currently in development for the treatment of hepatocellular and colon carcinomas. In vitro and in vivo studies were conducted to characterize the preclinical pharmacokinetics and
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