Tivozanib (AV-951)

For research use only.

Catalog No.S1207 Synonyms: KRN-951

20 publications

Tivozanib (AV-951) Chemical Structure

CAS No. 475108-18-0

Tivozanib (AV-951, KRN-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.

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10mM (1mL in DMSO) USD 240 In stock
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Selleck's Tivozanib (AV-951) has been cited by 20 publications

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Biological Activity

Description Tivozanib (AV-951, KRN-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.
Targets
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
EphB2 [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
PDGFRα [1]
(Cell-free assay)
6.5 nM 15 nM 24 nM 30 nM 40 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNuIFnDOVA:OC5|ODFOwG0> MVmyOFU5OzN3Nx?=

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[1]
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Kinase Assays:

Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1.
Cell Research:[1]
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  • Cell lines: Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts
  • Concentrations: 1 μM
  • Incubation Time: 15 minutes
  • Method: Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts-based assays are done to determine the ability of AV-951 to inhibit ligand-dependent phosphorylation of tyrosine kinase receptors. The cells are starved overnight in appropriate basic medium containing 0.5% fetal bovine serum (FBS). The cells are incubated for 1 hour following the addition of AV-951 or 0.1% DMSO, and then stimulated with the cognate ligand at 37 °C. Receptor phosphorylation is induced for 5 minutes except for VEGFR3 (10 minutes), c-Met (10 minutes), and c-Kit (15 minutes). All the ligands used in the assays are human recombinant proteins, except for VEGF-C, a rat recombinant protein. Following cell lysis, receptors are immunoprecipitated with appropriate antibodies and subjected to immunoblotting with phosphotyrosine. Quantification of the blots and calculation of IC50 values are carried ou
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: A549 xenografts in Athymic rats (RH-rnu/rnu)
  • Dosages: 1 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (43.96 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 454.86
Formula

C22H19ClN4O5

CAS No. 475108-18-0
Storage powder
in solvent
Synonyms KRN-951
Smiles CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03136627 Active not recruiting Drug: Tivozanib|Drug: Nivolumab Carcinoma Renal Cell AVEO Pharmaceuticals Inc.|Bristol-Myers Squibb March 22 2017 Phase 1|Phase 2
NCT01853644 Active not recruiting Drug: Tivozanib Recurrent Epithelial Ovarian Cancer|Recurrent Fallopian Tube Cancer|Recurrent Primary Peritoneal Cancer Northwestern University|National Comprehensive Cancer Network June 6 2013 Phase 2
NCT01834183 Withdrawn Drug: Tivozanib|Drug: Gemcitabine Renal Cell Carcinoma Dana-Farber Cancer Institute June 2013 Phase 2
NCT01807156 Terminated Drug: Tivozanib Hepatocellular Cancer Emory University|AVEO Pharmaceuticals Inc. March 2013 Phase 2
NCT01769885 Withdrawn Drug: tivozanib|Procedure: therapeutic conventional surgery Stage II Renal Cell Cancer|Stage III Renal Cell Cancer Roswell Park Cancer Institute|National Cancer Institute (NCI)|AVEO Pharmaceuticals Inc. March 14 2013 Not Applicable

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Would you please provide a little bit more detail regarding how to prepare the Tivozanib for in vivo treatment and the storage condition?

  • Answer:

    For in vivo formula, we recommend to use 2% DMSO+30% PEG 300+ddH2O up to 1mg/mL. Once dissolved it in solution, please make small aliquots and store them at -80C up to 6 months without repeated thawing and refreezing.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID