Home > VEGFR & VEGFR & > Brivanib Alaninate

Brivanib Alaninate

丙氨酸布立尼布,BMS-582664,BMS 582664,BMS582664

Brivanib alaninate是ATP竞争性VEGFR2抑制剂，IC50为25 nM，对VEGFR-1和FGFR-1的抑制性相对较弱，比对PDGFR-β的抑制性强超过240倍。

目录号
EY0896
EY0896
EY0896
纯度
99.44%
99.44%
99.44%
规格
1 mg
5 mg
10 mg
原价
510
1300
2420
售价
510
1300
2420
库存
现货
现货
现货
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  • 生物活性

    Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    276 nM

  • 动物实验

    90 mg/kg 口服

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Bhide RS, et al. J Med Chem, 2006, 49(7), 2143-2146.
    [2] Huynh H, 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, 14(19), 6146-6153.

    分子式
    C22H24FN5O4    		 分子量
    441.46    		 CAS号
    649735-63-7    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    88 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    88 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00437437 Tumors Drug: Brivanib Bristol-Myers Squibb Phase 1 2000-05-01 2013-06-20
    NCT01267253 Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma, Not Otherwise Specified|Persistent Disease|Recurrent Cervical Carcinoma Drug: Brivanib Alaninate|Other: Laboratory Biomarker Analysis Gynecologic Oncology Group|National Cancer Institute (NCI) Phase 2 2011-04-01 2017-01-26
    NCT00888173 Endometrial Adenocarcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Mixed Adenocarcinoma|Endometrial Mucinous Adenocarcinoma|Endometrial Serous Adenocarcinoma|Endometrial Squamous Cell Carcinoma|Endometrial Transitional Cell Carcinoma|Endometrial Undifferentiated Carcinoma|Recurrent Uterine Corpus Carcinoma Drug: Brivanib Alaninate|Other: Laboratory Biomarker Analysis Gynecologic Oncology Group|National Cancer Institute (NCI) Phase 2 2009-07-01 2016-03-16
    NCT00355238 Hepatocellular Carcinoma (HCC) Drug: brivanib (active) Bristol-Myers Squibb Phase 2 2006-12-01 2015-09-23
    NCT00437424 Carcinoma, Hepatocellular Drug: Brivanib Bristol-Myers Squibb Phase 1 2007-07-01 2011-05-03
    NCT00798252 Advanced Cancer Drug: Capecitabine|Drug: Doxorubicin|Drug: Ixabepilone|Drug: Docetaxel|Drug: Paclitaxel|Drug: Brivanib alaninate Bristol-Myers Squibb Phase 1 2009-03-01 2015-07-03
    NCT01540461 Hepatocellular Carcinoma Drug: Brivanib Bristol-Myers Squibb Phase 1 2012-03-01 2014-07-04
    NCT00435669 Tumors Drug: Brivanib|Drug: Brivanib Bristol-Myers Squibb Phase 1 2007-09-01 2009-01-21
    NCT00390936 Solid Tumors Drug: Brivanib Bristol-Myers Squibb Phase 1 2007-10-01 2011-01-24
    NCT01108705 Carcinoma, Hepatocellular Drug: Brivanib|Drug: Placebo Bristol-Myers Squibb Phase 3 2010-05-01 2015-09-23
    NCT00825955 Liver Cancer Drug: Brivanib|Other: Placebo|Procedure: Best Supportive Care Bristol-Myers Squibb Phase 3 2009-02-01 2017-03-03
    NCT01367275 Colorectal Cancer|Colorectal Adenocarcinoma Drug: Brivanib|Drug: Irinotecan M.D. Anderson Cancer Center|Bristol-Myers Squibb Phase 2 2011-08-01 2015-01-07
    NCT00640471 Colorectal Cancer Biological: cetuximab|Drug: brivanib alaninate NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 3 2008-05-01 2013-07-16
    NCT00633789 Advanced Non-small Cell Lung Cancer|Transitional Cell Carcinoma|Soft Tissue Sarcoma|Gastric/Esophageal Adenocarcinoma|Pancreatic Cancer Including Ampulla of Vater Drug: brivanib|Drug: Placebo Bristol-Myers Squibb Phase 2 2008-06-01 2015-09-23
    NCT00908752 Hepatocellular Carcinoma Drug: Brivanib|Other: Brivanib Placebo|Procedure: TACE Therapy Bristol-Myers Squibb Phase 3 2009-07-01 2017-03-03
    NCT01253668 Male and Female Subjects 18 Years of Age and Older With Metastatic Renal Cell Carcinoma. Eligible Patients Must Have Undergone and Failed Prior Treatment. Drug: Brivanib alaninate|Genetic: Polymerase chain reaction|Other: Iodine I 124 chimeric monoclonal antibody G250|Procedure: Positron emission tomography/computed tomography|Genetic: Protein expression analysis|Other: Immunohistochemistry Abramson Cancer Center of the University of Pennsylvania Phase 2 2010-11-01 2015-12-14
    NCT00858871 Hepato Cellular Carcinoma (HCC) Drug: Brivanib|Drug: Placebo|Drug: Sorafenib|Drug: Placebo Bristol-Myers Squibb Phase 3 2009-05-01 2016-10-14
    NCT00207051 Colorectal Cancer Drug: Brivanib + Cetuximab Bristol-Myers Squibb Phase 1 2006-01-01 2011-01-24
    NCT00300027 Gastrointestinal Neoplasms Drug: BMS-582664 Bristol-Myers Squibb Phase 1 2006-04-01 2010-02-27
    NCT01046864 Gastro-Intestinal Cancer Drug: 5-FU|Drug: Leucovorin|Drug: 5-FU|Drug: Irinotecan|Drug: Brivanib|Drug: Brivanib|Drug: Brivanib Bristol-Myers Squibb Phase 1 2010-02-01 2014-09-15
    NCT00207103 Tumors|Neoplasm Metastasis Drug: Brivanib|Drug: Brivanib|Drug: Brivanib|Drug: Brivanib|Drug: Brivanib|Drug: Brivanab Bristol-Myers Squibb Phase 1 2004-09-01 2008-11-03
    NCT00594984 Metastatic Colorectal Cancer (MCRC) Drug: Cetuximab|Drug: Irinotecan|Drug: Brivanib|Drug: Brivanib|Drug: Brivanib Placebo Bristol-Myers Squibb Phase 1|Phase 2 2008-05-01 2015-10-12

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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