Brivanib (alaninate)

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Chemical Structure| 649735-63-7 同义名 : Brivanib alaninate; BMS-582664
CAS号 : 649735-63-7
货号 : A369272
分子式 : C22H24FN5O4
纯度 : 99%+
分子量 : 441.46
MDL号 : MFCD22577162
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(237.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

0.5% methylcellulose+0.2% Tween 80+water 10 mg/mL suspension

生物活性
描述 Brivanib alaninate is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00594984 Metastatic Colorectal Cancer (... 展开 >>MCRC) 收起 << Phase 1 Phase 2 Completed - United States, California ... 展开 >> Usc/Norris Comprehensive Cancer Center Hospital Los Angeles, California, United States, 90033 Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Kentucky James Graham Brown Cancer Center Louisville, Kentucky, United States, 40202 United States, Missouri Washington University Saint Louis, Missouri, United States, 63110 Argentina Local Institution Buenos Aires, Argentina, C1426ANZ Denmark Local Institution Odense C, Denmark, 5000 Italy Local Institution Meldola Fc, Italy, 47014 Local Institution Milano, Italy, 20141 Korea, Republic of Local Institution Seoul, Korea, Republic of, 135-710 Spain Local Institution Madrid, Spain, 28050 Sweden Local Institution Stockholm, Sweden, 17176 Local Institution Uppsala, Sweden, 75185 收起 <<
NCT00300027 Gastrointestinal Neoplasms Phase 1 Terminated - United States, Arkansas ... 展开 >> Local Institution Little Rock, Arkansas, United States United States, California Local Institution Los Angeles, California, United States United States, District of Columbia Local Institution Washington, District of Columbia, United States United States, Iowa Local Institution Iowa City, Iowa, United States United States, North Carolina Local Institution Durham, North Carolina, United States United States, Texas Local Institution Temple, Texas, United States 收起 <<
NCT00207103 Tumors Neopla... 展开 >>sm Metastasis 收起 << Phase 1 Completed - United States, California ... 展开 >> Premiere Oncology Santa Monica, California, United States, 90404 United States, Indiana Indiana University Med Center Indianapolis, Indiana, United States, 46202 United States, Wisconsin University Of Wisconsin Comprehensive Center Madison, Wisconsin, United States, 53792 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Ottawa, Ontario, Canada, K1H 1C4 Italy Local Institution Milano, Italy, 20141 United Kingdom Local Institution Middlesex, Greater London, United Kingdom, HA6 2RN Local Institution Manchester, Greater Manchester, United Kingdom, M20 4BX 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.33mL

2.27mL

1.13mL

22.65mL

4.53mL

2.27mL
参考文献

[1]Huynh H, Ngo VC, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res. 2008 Oct 1;14(19):6146-53.

[2]Bhide RS, Cai ZW, et al. Discovery and preclinical studies of (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), an in vivo active potent VEGFR-2 inhibitor. J Med Chem. 2006 Apr 6;49(7):2143-6.