Home > VEGFR & VEGFR & > Brivanib

Brivanib

布立尼布,BMS-540215,BMS 540215,BMS540215

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

目录号
EY1027
EY1027
EY1027
纯度
99.39%
99.39%
99.39%
规格
1 mg
5 mg
10 mg
原价
490
990
1800
售价
490
990
1800
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Brivanib 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. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10 μM 左右

  • 动物实验

    60 mg/kg(口服)或10 mg/kg(静脉注射)口服或静脉注射

  • 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.

    分子式
    C19H19FN4O3    		 分子量
    370.38    		 CAS号
    649735-46-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    75 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    3 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
    NCT01540461 Hepatocellular Carcinoma Drug: Brivanib Bristol-Myers Squibb Phase 1 2012-03-01 2014-07-04
    NCT00437424 Carcinoma, Hepatocellular Drug: Brivanib Bristol-Myers Squibb Phase 1 2007-07-01 2011-05-03
    NCT00355238 Hepatocellular Carcinoma (HCC) Drug: brivanib (active) Bristol-Myers Squibb Phase 2 2006-12-01 2015-09-23
    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
    NCT01108705 Carcinoma, Hepatocellular Drug: Brivanib|Drug: Placebo Bristol-Myers Squibb Phase 3 2010-05-01 2015-09-23
    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
    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
    NCT00825955 Liver Cancer Drug: Brivanib|Other: Placebo|Procedure: Best Supportive Care Bristol-Myers Squibb Phase 3 2009-02-01 2017-03-03
    NCT00435669 Tumors Drug: Brivanib|Drug: Brivanib Bristol-Myers Squibb Phase 1 2007-09-01 2009-01-21
    NCT00908752 Hepatocellular Carcinoma Drug: Brivanib|Other: Brivanib Placebo|Procedure: TACE Therapy Bristol-Myers Squibb Phase 3 2009-07-01 2017-03-03
    NCT00390936 Solid Tumors Drug: Brivanib Bristol-Myers Squibb Phase 1 2007-10-01 2011-01-24
    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
    NCT00640471 Colorectal Cancer Biological: cetuximab|Drug: brivanib alaninate NCIC Clinical Trials Group|Canadian Cancer Trials Group Phase 3 2008-05-01 2013-07-16
    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
    NCT00858871 Hepato Cellular Carcinoma (HCC) Drug: Brivanib|Drug: Placebo|Drug: Sorafenib|Drug: Placebo Bristol-Myers Squibb Phase 3 2009-05-01 2016-10-14
    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
    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
    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
    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
    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

    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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