Home > VEGFR & VEGFR & > Linifanib

Linifanib

RG3635,RG 3635,RG-3635,ABT 869,ABT869,ABT-869,AL-39324

Linifanib是一种新型，有效，ATP竞争性VEGFR/PDGFR抑制剂，同时抑制KDR， CSF-1R， Flt-1/3和PDGFRβ，其IC50分别为4 nM， 3 nM， 3 nM/4 nM和66 nM ，对具有突变激酶依赖性的癌细胞（即FLT3）最有效。

目录号
EY1828
EY1828
EY1828
EY1828
纯度
99.63%
99.63%
99.63%
99.63%
规格
5 mg
10 mg
50 mg
100 mg
原价
490
780
1980
3320
售价
490
780
1980
3320
库存
现货
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0-100 μM

  • 动物实验

    ~ 10 mg/kg 口服处理

  • 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] Albert DH, et al. Mol Cancer Ther, 2006, 5(4), 995-1006.
    [2] Zhou, J., et al. 2009. J Hematol Oncol. 2: 33. PMID: 19642998
    [3] Shankar, D.B., et al. 2007. Blood. 109: 3400-3408. PMID: 17209055

    分子式
    C21H18FN5O    		 分子量
    375.4    		 CAS号
    796967-16-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥70 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 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
    NCT01381341 Advanced Solid Tumors Drug: linifanib Abbott Phase 1 2011-05-01 2012-03-21
    NCT01401933 Advanced Solid Tumors Drug: Linifanib|Drug: Rifampin Abbott Phase 1 2011-05-01 2011-10-31
    NCT01413893 Advanced Solid Tumors Drug: linifanib Abbott Phase 1 2011-06-01 2012-08-01
    NCT01506934 Advanced or Metastatic Solid Tumors Drug: linifanib Abbott Phase 1 2011-10-01 2012-08-24
    NCT01365910 Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Drug: linifanib Vanderbilt-Ingram Cancer Center Phase 2 2011-06-01 2014-08-24
    NCT01114191 Solid Tumors Drug: ABT-869|Drug: ketoconazole Abbott Phase 1 2010-05-01 2011-07-22
    NCT01286974 Advanced Solid Tumors Drug: [14C]linifanib|Drug: ABT-869, linifanib Abbott Phase 1 2011-08-01 2012-09-19
    NCT01225302 Non-Small Cell Lung Cancer Drug: Linifanib|Drug: Linifanib|Drug: Carboplatin|Drug: Paclitaxel Abbott Phase 1 2010-09-01 2012-07-13
    NCT00517790 Non-Small Cell Lung Cancer (NSCLC) Drug: ABT-869 .25 mg/kg|Drug: ABT-869 0.10 mg/kg AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2007-08-01 2013-03-29
    NCT01009593 Hepatocellular Carcinoma Non-resectable|Hepatocellular Carcinoma Recurrent|Carcinoma, Hepatocellular|Liver Diseases|Neoplasms by Histologic Type|Digestive System Neoplasms|Carcinoma|Liver Neoplasms|Neoplasms|Neoplasms by Site|Digestive System Diseases|Adenocarcinoma|Neoplasms, Glandular and Epithelial Drug: ABT-869|Drug: Sorafenib Abbott Phase 3 2010-01-01 2012-09-07
    NCT00517920 Advanced Hepatocellular Carcinoma Drug: ABT-869 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2007-09-01 2013-01-02
    NCT00645177 Metastatic Breast Cancer Drug: ABT-869|Drug: paclitaxel|Drug: Placebo for ABT-869 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2008-07-01 2013-01-23
    NCT00718380 Solid Tumor Drug: ABT-869 Abbott Phase 1 2008-09-01 2012-07-13
    NCT00733187 Advanced Solid Tumors Drug: ABT-869 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 1 2009-02-01 2013-02-07
    NCT00486538 Advanced Renal Cell Carcinoma Drug: ABT-869 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2007-06-01 2013-01-02
    NCT00716534 Advanced or Metastatic Non-Small Cell Lung Cancer Drug: ABT-869|Drug: Placebo for ABT-869|Drug: ABT-869|Drug: Carboplatin|Drug: Paclitaxel AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2008-06-01 2013-04-19
    NCT00754104 Solid Tumors Drug: ABT-869|Drug: Tarceva Abbott|Genentech, Inc. Phase 1 2008-09-01 2011-01-17
    NCT00707889 Advanced Colorectal Cancer|Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum Drug: ABT-869|Drug: bevacizumab|Drug: oxaliplatin|Drug: folinic acid|Drug: fluorouracil|Drug: ABT-869 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Phase 2 2008-10-01 2013-05-07

    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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