1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Tivozanib (Synonyms: AV-951)

Cat. No.: HY-10977 Purity: 99.46%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
Tivozanib Chemical Structure

Tivozanib Chemical Structure

CAS No. : 475108-18-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $66 In-stock
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10 mg $85 In-stock
50 mg $240 In-stock
100 mg $420 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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. IC50 value: 30 nM/6.5 nM/15 nM(VEGFR1/2/3) [1] Target: VEGFR1/2/3 in vitro: AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells [1]. In vivo studies show that AV-951 also decreases the micro vessel density and suppresses VEGFR2 phosphorylation levels in tumor xenografts, especially at a concentration of 1mg/kg (p.o. administration). AV-951 shows almost complete inhibition of tumor xenografts growth (TGI>85%) in athymic rats [1]. Another study in rat peritoneal disseminated tumor model shows that AV-951 could prolong the survival of the tumor-bearing rats with the MST of 53.5 days. AV-951 displays antitumor activity against many human tumor xenografts including lung, breast, colon, ovarian, pancreas and prostate cancer [2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00826878 AVEO Pharmaceuticals, Inc. Carcinoma, Non-Small-Cell Lung January 2009 Phase 1
NCT00563147 AVEO Pharmaceuticals, Inc. Renal Cell Carcinoma November 2007 Phase 1
NCT00717340 AVEO Pharmaceuticals, Inc. Metastatic Breast Cancer February 2009 Phase 1
NCT00660153 AVEO Pharmaceuticals, Inc. Colorectal Cancer|Gastrointestinal Cancer June 2008 Phase 1
NCT00502307 AVEO Pharmaceuticals, Inc. Carcinoma, Renal Cell October 2007 Phase 2
NCT01306630 AVEO Pharmaceuticals, Inc. Advanced Solid Tumors|Locally Advanced or Metastatic Breast or Colorectal Cancer November 2010 Phase 1
NCT01030783 AVEO Pharmaceuticals, Inc. Advanced Renal Cell Carcinoma December 2009 Phase 3
NCT01369433 AVEO Pharmaceuticals, Inc. Solid Tumors June 2010
NCT00826878 AVEO Pharmaceuticals, Inc. Carcinoma, Non-Small-Cell Lung January 2009 Phase 1
NCT00563147 AVEO Pharmaceuticals, Inc. Renal Cell Carcinoma November 2007 Phase 1
NCT00717340 AVEO Pharmaceuticals, Inc. Metastatic Breast Cancer February 2009 Phase 1
NCT00660153 AVEO Pharmaceuticals, Inc. Colorectal Cancer|Gastrointestinal Cancer June 2008 Phase 1
NCT00502307 AVEO Pharmaceuticals, Inc. Carcinoma, Renal Cell October 2007 Phase 2
NCT01306630 AVEO Pharmaceuticals, Inc. Advanced Solid Tumors|Locally Advanced or Metastatic Breast or Colorectal Cancer November 2010 Phase 1
NCT01030783 AVEO Pharmaceuticals, Inc. Advanced Renal Cell Carcinoma December 2009 Phase 3
NCT01369433 AVEO Pharmaceuticals, Inc. Solid Tumors June 2010
NCT01316848 AVEO Pharmaceuticals, Inc. Food Effect of Tivozanib in Health Subjects February 2011 Phase 1
NCT03136627 AVEO Pharmaceuticals, Inc.|Bristol-Myers Squibb Carcinoma, Renal Cell March 22, 2017 Phase 1|Phase 2
NCT01807156 Emory University|AVEO Pharmaceuticals, Inc. Hepatocellular Cancer March 2013 Phase 2
NCT01363778 AVEO Pharmaceuticals, Inc. Healthy May 2011 Phase 1
NCT01363804 AVEO Pharmaceuticals, Inc. Healthy May 2011 Phase 1
NCT01834183 Dana-Farber Cancer Institute Renal Cell Carcinoma June 2013 Phase 2
NCT01853644 Northwestern University|National Comprehensive Cancer Network Recurrent Epithelial Ovarian Cancer|Recurrent Fallopian Tube Cancer|Recurrent Primary Peritoneal Cancer May 2013 Phase 2
NCT01769885 Roswell Park Cancer Institute|National Cancer Institute (NCI)|AVEO Pharmaceuticals, Inc. Stage II Renal Cell Cancer|Stage III Renal Cell Cancer March 14, 2013
NCT01297244 AVEO Pharmaceuticals, Inc. Renal Cell Carcinoma January 2011 Phase 2
NCT01972516 Dana-Farber Cancer Institute|National Comprehensive Cancer Network|AVEO Pharmaceuticals, Inc. Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma November 2013 Phase 2
NCT01846871 Massachusetts General Hospital|National Comprehensive Cancer Network Glioblastoma June 2013 Phase 2
NCT01673386 AVEO Pharmaceuticals, Inc.|Astellas Pharma Inc Metastatic Renal Cell Carcinoma July 2012 Phase 2
NCT01210846 AVEO Pharmaceuticals, Inc. Advanced Solid Tumors October 2010 Phase 1
NCT01076010 AVEO Pharmaceuticals, Inc. Advanced Renal Cell Carcinoma March 2010 Phase 3
NCT01782313 Northwestern University|AVEO Pharmaceuticals, Inc. Recurrent Adult Soft Tissue Sarcoma|Stage III Adult Soft Tissue Sarcoma|Stage IV Adult Soft Tissue Sarcoma February 2013 Phase 2
NCT01835223 Roswell Park Cancer Institute|National Comprehensive Cancer Network|AVEO Pharmaceuticals, Inc.|National Cancer Institute (NCI) Advanced Adult Hepatocellular Carcinoma|Non-Resectable Hepatocellular Carcinoma July 11, 2013 Phase 1|Phase 2
NCT02627963 AVEO Pharmaceuticals, Inc. Carcinoma, Renal Cell April 2016 Phase 3
NCT01728181 University of Utah Non-small Cell Lung Cancer|Stage IV Disease|EGFR Unknown or Wild-type November 2013 Phase 1|Phase 2
NCT01745367 AVEO Pharmaceuticals, Inc.|Astellas Pharma Inc Triple Negative Breast Cancer November 2012 Phase 2
NCT01885949 Massachusetts General Hospital|National Comprehensive Cancer Network Prostate Cancer June 2013 Phase 2
NCT01478594 AVEO Pharmaceuticals, Inc. Colorectal Cancer December 2011 Phase 2
NCT01631097 AVEO Pharmaceuticals, Inc. Hepatic Impairment May 2012 Phase 1
NCT01058655 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Novartis|AVEO Pharmaceuticals, Inc. Gastrointestinal Cancer February 2010 Phase 1|Phase 2
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References
Molecular Weight

454.86

Formula

C₂₂H₁₉ClN₄O₅

CAS No.

475108-18-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Tivozanib
Cat. No.:
HY-10977
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