Catalog No.S1207 Synonyms: KRN-951
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.
Cited by 7 Publications
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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.
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.
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|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.|
AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells. 
|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.  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. |
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.
|In vitro||DMSO||20 mg/mL (43.96 mM)|
|In vivo||0.5% methylcellulose||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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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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