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    Tivozanib (AV951; KRN-951)
    Tivozanib (AV951; KRN-951)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0505
    CAS #: 475108-18-0Purity ≥98%

    Description: Tivozanib (formerly KRN951 or AV-951; brand name Fotivda) is a novel, orally bioavailable, potent and selective inhibitor of VEGFR (vascular endothelial growth factor receptors) with potential antineoplastic activity. It inhibits VEGFR1/2/3 with IC50s of 30 nM/6.5 nM/15 nM. Tivozanib was approved by European Medicines Agency (EMA)  in August 2017 and US FDA in March 2021 for the treatment of relapsed or refractory advanced renal cell carcinoma (RCC). Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGF plays a key role in tumor angiogenesis by stimulating the proangiogenic signaling of endothelial cells via activation of VEGF receptor (VEGFR) tyrosine kinases. Therefore, VEGFRs are an attractive therapeutic target for cancer treatment and Tivozanib has the potential to be used as an anticancer agent.

    References: Cancer Res. 2006 Sep 15;66(18):9134-42; Cancer Sci. 2008 Mar;99(3):623-30.

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    Molecular Weight (MW)454.86
    CAS No.475108-18-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 20 mg/mL (43.96 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)0.5% methylcellulose: 30 mg/mL
    SynonymsTivozanib; KRN-951, AV-951; AV951; AV 951; KRN951; KRN 951 

    Chemical Name: 1-(2-chloro-4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-3-(5-methylisoxazol-3-yl)urea

    SMILES Code: O=C(NC1=NOC(C)=C1)NC2=CC=C(OC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2Cl

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    In Vitro

    In vitro activity: Tivozanib (AV-951) is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells. Tivozanib potently inhibits VEGF-induced VEGFR2 phosphorylation in endothelial cells with IC50 of 0.16 nM. It also inhibits ligand-induced phosphorylation of PDGFRβ and c-Kit with IC50 of 1.72 and 1.63 nM, respectively. Tivozanib inhibits VEGF-mediated migration of human umbilical vein endothelial cells

    Kinase Assay: 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 Assay: 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 out.

    In VivoIn 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.
    Animal modelA549 xenografts in Athymic rats (RH-rnu/rnu)
    Formulation & DosageFormulated in 0.5% methylcellulose in distilled water; 1mg/kg; oral gavage
    ReferencesCancer Res. 2006 Sep 15;66(18):9134-42; Cancer Sci. 2008 Mar;99(3):623-30.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Tivozanib (AV-951)

    Effects of KRN951 on VEGFR-2 phosphorylation levels on tumor endothelium and tumor microvessel density.  2006 Sep 15;66(18):9134-42.

    Tivozanib (AV-951)

    DCE-MRI analysis of tumor vascular permeability. Athymic rats bearing Calu-6 tumors were randomized at day −1 and then treated with 0.2 mg/kg KRN951 (○), 1 mg/kg KRN951 (▴), or vehicle (•) once daily for 14 days (days 0-13).  2006 Sep 15;66(18):9134-42.

    Tivozanib (AV-951)

    Effects of KRN951 on tumor vessel diameter and pericyte coverage.  2006 Sep 15;66(18):9134-42.


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