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Merck
CN

SML3671

Brivanib

≥98% (HPLC)

别名:

BMS-540215, (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-582664 active drug, BMS540215, BMS582664 active drug

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关于此项目

经验公式（希尔记法）:
C19H19FN4O3
化学文摘社编号:
649735-46-6
分子量:
370.38
UNSPSC Code:
12352200
NACRES:
NA.25
MDL number:
MFCD13194684

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SMILES string

Fc1c2c([nH]c(c2)C)ccc1Oc3ncn[n]4c3c(c(c4)OC[C@H](O)C)C

InChI

1S/C19H19FN4O3/c1-10-6-13-14(23-10)4-5-15(17(13)20)27-19-18-12(3)16(26-8-11(2)25)7-24(18)22-9-21-19/h4-7,9,11,23,25H,8H2,1-3H3/t11-/m1/s1

InChI key

WCWUXEGQKLTGDX-LLVKDONJSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

相关类别

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).
Orally active, ATP-competitive FGF & VEGF receptor tyrosine kinase inhibitor with antitumor efficacy in vivo.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000239089
0000239090
0000230413
0000239089
0000239090

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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
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
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

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