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Tivozanib

KRN-951,KRN 951,KRN951,AV951,AV 951,AV-951,

Tivozanib是VEGFR抑制剂，对VEGFR1，2和3的IC50分别为30 nM，6.5 nM和15 nM，还能抑制PDGFR和c-Kit，对FGFR-1，Flt3，c-Met，EGFR和IGF-1R的抑制性较低。

目录号
EY0358
EY0358
EY0358
EY0358
纯度
99.55%
99.55%
99.55%
99.55%
规格
1 mg
5 mg
10 mg
50 mg
原价
260
640
960
2860
售价
260
640
960
2860
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    Tivozanib (AV-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    1 μM

  • 动物实验

    1 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] Nakamura K, et al. Cancer Res, 2006, 66(18), 9134-9142.
    [2] C Lance Cowey. Profile of tivozanib and its potential for the treatment of advanced renal cell carcinoma. Drug Des Devel Ther. 2013; 7: 519–527. Published online 2013 Jun 21. doi: 10.2147/DDDT.S31442.
    [3] Brian M,et al. Multicenter Phase II Study of Tivozanib (AV-951) and Everolimus (RAD001) for Patients With Refractory, Metastatic Colorectal Cancer. Oncologist. 2013 Apr; 18(4): 377–378. Published online 2013 Apr 11. doi: 10.1634/theoncologist.2012-0378.
    [4] Mehmet Hepgur,et al. Tivozanib in the treatment of renal cell carcinoma. Biologics. 2013; 7: 139–148. Published online 2013 Jun 11. doi: 10.2147/BTT.S32958.

    分子式
    C22H19ClN4O5    		 分子量
    454.86    		 CAS号
    475108-18-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    20 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

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

    NCT01316848 Food Effect of Tivozanib in Health Subjects Drug: tivozanib AVEO Pharmaceuticals, Inc. Phase 1 2011-02-01 2012-06-01
    NCT01807156 Hepatocellular Cancer Drug: Tivozanib Emory University|AVEO Pharmaceuticals, Inc. Phase 2 2013-03-01 2016-03-22
    NCT01363778 Healthy Drug: tivozanib AVEO Pharmaceuticals, Inc. Phase 1 2011-05-01 2012-06-01
    NCT01363804 Healthy Drug: Tivozanib AVEO Pharmaceuticals, Inc. Phase 1 2011-05-01 2012-06-01
    NCT01834183 Renal Cell Carcinoma Drug: Tivozanib|Drug: Gemcitabine Dana-Farber Cancer Institute Phase 2 2013-06-01 2013-06-17
    NCT00826878 Carcinoma, Non-Small-Cell Lung Drug: Tivozanib (AV-951) AVEO Pharmaceuticals, Inc. Phase 1 2009-01-01 2012-06-27
    NCT00563147 Renal Cell Carcinoma Drug: tivozanib (AV-951) plus temsirolimus AVEO Pharmaceuticals, Inc. Phase 1 2007-11-01 2011-09-30
    NCT01306630 Advanced Solid Tumors|Locally Advanced or Metastatic Breast or Colorectal Cancer Drug: tivozanib (AV-951) and capecitabine (Xeloda庐) AVEO Pharmaceuticals, Inc. Phase 1 2010-11-01 2014-01-23
    NCT00717340 Metastatic Breast Cancer Drug: tivozanib (AV-951) + paclitaxel AVEO Pharmaceuticals, Inc. Phase 1 2009-02-01 2012-06-27
    NCT01853644 Recurrent Epithelial Ovarian Cancer|Recurrent Fallopian Tube Cancer|Recurrent Primary Peritoneal Cancer Drug: Tivozanib Northwestern University|National Comprehensive Cancer Network Phase 2 2013-05-01 2017-02-19
    NCT00660153 Colorectal Cancer|Gastrointestinal Cancer Drug: Tivozanib (AV-951) plus FOLFOX6 AVEO Pharmaceuticals, Inc. Phase 1 2008-06-01 2012-08-24
    NCT01769885 Stage II Renal Cell Cancer|Stage III Renal Cell Cancer Drug: tivozanib|Procedure: therapeutic conventional surgery Roswell Park Cancer Institute|National Cancer Institute (NCI)|AVEO Pharmaceuticals, Inc. 2013-03-01 2013-12-17
    NCT01297244 Renal Cell Carcinoma Drug: Tivozanib AVEO Pharmaceuticals, Inc. Phase 2 2011-01-01 2013-11-04
    NCT01972516 Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Drug: Tivozanib Dana-Farber Cancer Institute|National Comprehensive Cancer Network|AVEO Pharmaceuticals, Inc. Phase 2 2013-11-01 2016-08-10
    NCT01846871 Glioblastoma Drug: Tivozanib Massachusetts General Hospital|National Comprehensive Cancer Network Phase 2 2013-06-01 2016-12-01
    NCT01673386 Metastatic Renal Cell Carcinoma Drug: Tivozanib Hydrochloride|Drug: Sunitinib AVEO Pharmaceuticals, Inc.|Astellas Pharma Inc Phase 2 2012-07-01 2015-06-22
    NCT01210846 Advanced Solid Tumors Drug: tivozanib AVEO Pharmaceuticals, Inc. Phase 1 2010-10-01 2011-09-23
    NCT01030783 Advanced Renal Cell Carcinoma Drug: tivozanib (AV-951)|Drug: Sorafenib AVEO Pharmaceuticals, Inc. Phase 3 2009-12-01 2014-02-19
    NCT01076010 Advanced Renal Cell Carcinoma Drug: Tivozanib|Drug: Sorafenib AVEO Pharmaceuticals, Inc. Phase 3 2010-03-01 2015-06-22
    NCT00502307 Carcinoma, Renal Cell Drug: Tivozanib (AV-951)|Drug: Placebo comparator AVEO Pharmaceuticals, Inc. Phase 2 2007-10-01 2012-10-02
    NCT01782313 Recurrent Adult Soft Tissue Sarcoma|Stage III Adult Soft Tissue Sarcoma|Stage IV Adult Soft Tissue Sarcoma Drug: tivozanib|Other: laboratory biomarker analysis Northwestern University|AVEO Pharmaceuticals, Inc. Phase 2 2013-02-01 2016-03-09
    NCT01369433 Solid Tumors Drug: tivozanib (AV-951) + paclitaxel|Drug: tivozanib (AV-951) + temsirolimus|Drug: tivozanib (AV-951)|Drug: tivozanib (AV-951)|Drug: tivozanib (AV-951) + capecitabine|Drug: tivozanib (AV-951) AVEO Pharmaceuticals, Inc. 2010-06-01 2015-06-22
    NCT01835223 Advanced Adult Hepatocellular Carcinoma|Non-Resectable Hepatocellular Carcinoma Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Tivozanib Roswell Park Cancer Institute|National Comprehensive Cancer Network|AVEO Pharmaceuticals, Inc.|National Cancer Institute (NCI) Phase 1|Phase 2 2013-07-11 2017-02-22
    NCT02627963 Carcinoma, Renal Cell Drug: tivozanib hydrochloride|Drug: Sorafenib AVEO Pharmaceuticals, Inc. Phase 3 2016-04-01 2017-03-06
    NCT01728181 Non-small Cell Lung Cancer|Stage IV Disease|EGFR Unknown or Wild-type Drug: Tivozanib|Drug: Erlotinib|Other: Standard of Care treatment University of Utah Phase 1|Phase 2 2013-11-01 2013-07-23
    NCT01745367 Triple Negative Breast Cancer Drug: Tivozanib Hydrochloride|Drug: paclitaxel AVEO Pharmaceuticals, Inc.|Astellas Pharma Inc Phase 2 2012-11-01 2015-06-22
    NCT01885949 Prostate Cancer Drug: Tivozanib|Drug: Enzalutamide Massachusetts General Hospital|National Comprehensive Cancer Network Phase 2 2013-06-01 2016-12-21
    NCT01478594 Colorectal Cancer Drug: Tivozanib|Drug: Bevacizumab|Drug: mFOLFOX6 AVEO Pharmaceuticals, Inc. Phase 2 2011-12-01 2015-06-09
    NCT01631097 Hepatic Impairment Drug: Tivozanib hydrochloride AVEO Pharmaceuticals, Inc. Phase 1 2012-05-01 2014-01-23
    NCT00970411 Solid Tumors Drug: KRN951 Kyowa Hakko Kirin Co., Ltd Phase 1 2009-08-01 2017-01-03
    NCT01058655 Gastrointestinal Cancer Drug: RAD001|Drug: AV-951 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Novartis|AVEO Pharmaceuticals, Inc. Phase 1|Phase 2 2010-02-01 2016-01-21

    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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