Tivozanib (AV-951)

Catalog No.S1207 Synonyms: KRN-951

Tivozanib (AV-951) Chemical Structure

Molecular Weight(MW): 454.86

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.

Size Price Stock Quantity  
In DMSO USD 240 In stock
USD 120 In stock
USD 170 In stock
USD 570 In stock
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5 Customer Reviews

  • On-chip angiogenesis assay. Fluorescence imaging of Tg(fli1a:EGFP) embryos at 64 hpf. Transgenic embryos were arrayed and immobilized at 16 hpf and continuously perfused with E3 media containing vehicle control (dimethyl sulfoxide) or selected small-molecule antiangiogenic drugs (Sunitinib and Tivozanib). Right panel: microscopic visualization of patterns of ISV. White arrows: normal ISV growth; blue arrows: partial ISV growth inhibition; and red arrows; complete ISV growth inhibition.

    Cytometry A 2014 85(6), 537-47. Tivozanib (AV-951) purchased from Selleck.

    After serum-starvation for 24 h, the MCF7 cells were co-treated with 10 nM TPA and the indicated doses VEGFR inhibitor, Tivozanib, for 24 h. The levels of fibronectin, p-PKC-α, p-ERK, p-AKT, t-AKT and β-actin protein expression were analyzed by western blotting. The levels of fibronectin mRNA were analyzed by real-time PCR. The results are representative of three independent experiments. The values shown are the means ±SEM. * P < 0.05, ** P < 0.01 vs. control. # P < 0.05, ## P < 0.01 vs. TPA-treated cells. Con: control. LY: LY294002, U: UO126, Go: Go6983, Akt IV: Akt IV inhibitor.

    Cell Physiol Biochem 2013 32(5), 1541-50. Tivozanib (AV-951) purchased from Selleck.

  • Effects of VEGFR inhibitor tivozanib treatment on ALP activity (A, 48 h after loading), Runx2 (B, 6 h after loading) and Col-1 (C, 48 h after loading) mRNA expression (the amount of decrease compared to untreated groups and the significant difference were marked, *p < 0.05).

    Arch Biochem Biophys, 2016, 607:37-43. Tivozanib (AV-951) purchased from Selleck.

     

    Reversal effect of Tivozanib on the sensitivity of HEK/ABCB1 cells to vincrstine. The figure showes the survival curves of cells at different concentrations of vincristine with or without Tivozanib. Cell viability was determined by MTT Assay. HEK293 is human embryonic kidney cell line while HEK/ABCB1 is ABCB1-transfected cell line. Verapamil was used as a positive control of ABCB1 inhibitor.

    Tivozanib (AV-951) purchased from Selleck.

  •  

    Figure 7 shows the effect of Tivozanib on the accumulation of [3H]-mitoxantrone. The accumulation of [3H]-mitoxantrone in empty vector transfected HEK293/pcDNA3.1, ABCG2 vector transfected wild-type ABCG2-482-R2, mutant ABCG2-482-G2 and mutant ABCG2-482-T7 cells was measured by the Accumulation Assays. Columns are the mean of triplicate determinations; bars, SD. *P<0.05, **P<0.01 versus the control group. Fumitremorgin C (FTC) was used as a positive control of ABCG2 inhibitor.

    Tivozanib (AV-951) purchased from Selleck.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

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. 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 NV:5bZJYWHKxbHnm[ZJifGmxbjDhd5NigQ>? NI\Q[JdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOsJGlEPTB;MD6zPEDPxE1? NIGxWFgzPDV6M{O1Oy=>

... 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)
  • Formulation: 0.5% methylcellulose in distilled water
  • 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 individually and in order:
0.5% methylcellulose
30 mg/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
Synonyms KRN-951

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02627963 Recruiting Carcinoma, Renal Cell AVEO Pharmaceuticals, Inc. April 2016 Phase 3
NCT01972516 Terminated Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Dana-Farber Cancer Institute|National Comprehensive Cancer Network|AVEO Pharmaceuticals, Inc. November 2013 Phase 2
NCT01728181 Withdrawn Non-small Cell Lung Cancer|Stage IV Disease|EGFR Unknown or Wild-type University of Utah November 2013 Phase 1|Phase 2
NCT01835223 Recruiting Advanced Adult Hepatocellular Carcinoma|Non-Resectable Hepatocellular Carcinoma Roswell Park Cancer Institute|National Comprehensive Cancer Network|AVEO Pharmaceuticals, Inc.|National Cancer Institute (NCI) July 2013 Phase 1|Phase 2
NCT01885949 Active, not recruiting Prostate Cancer Massachusetts General Hospital|National Comprehensive Cancer Network June 2013 Phase 2
NCT01846871 Completed Glioblastoma Massachusetts General Hospital|National Comprehensive Cancer Network June 2013 Phase 2

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID