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Tivozanib hydrate  (Synonyms: AV-951 hydrate; KRN951 hydrate)

Cat. No.: HY-112467 Purity: 99.0%
Handling Instructions Technical Support

Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy.

For research use only. We do not sell to patients.

CAS No. : 682745-40-0

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Tivozanib hydrate:

Top Publications Citing Use of Products

    Tivozanib hydrate purchased from MedChemExpress. Usage Cited in: Angiogenesis. 2025 Feb 3;28(2):13.  [Abstract]

    Western blots showing VEGFR2 and β-actin expression in HUVECs that were pre-treated with 4 µg/mL IgG, 4 µg/mL anti-VEGFR2 NAb, 0.1% DMSO (vehicle), 100 nM Lenvatinib, 250 nM Tivozanib, or 1 mM ATP for 2 h and then exposed to 0.1% DMSO or 10 µM Clioquinol for another 4 h.

    Tivozanib hydrate purchased from MedChemExpress. Usage Cited in: Angiogenesis. 2025 Feb 3;28(2):13.  [Abstract]

    Western blots showing p-VEGFR2, VEGFR2, and β-actin expression in HUVECs that were treated with 0.1% DMSO, 100 nM Lenvatinib, 250 nM Tivozanib or 10 µM Clioquinol for 1 h and then stimulated with 25 ng/mL VEGF for 7 min.

    Tivozanib hydrate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2023 Feb 14;16(2):295.

    Effect of tivozanib and losartan on survival rate, body weight, urine flow and urine protein levels. Mice either daily received tivozanib (1 mg/kg), Tivozanib plus Losartan (10 mg/kg; Tivo + Los10), Tivozanib plus Losartan (30 mg/kg; Tivo + Los30) or vehicle control.Probability of survival.

    Tivozanib hydrate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2023 Feb 14;16(2):295.

    Effect of tivozanib and losartan on histology of heart and kidney. Mice either daily received Tivozanib (1 mg/kg), Tivozanib plus losartan (10 mg/kg; Tivo + Los10), Tivozanib plus losartan (30 mg/kg; Tivo + Los30) or vehicle control. Photomicrographs of mice aorta.

    Tivozanib hydrate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2023 Feb 14;16(2):295.

    Mice either daily received Tivozanib (1 mg/kg), Tivozanib plus losartan (10 mg/kg; Tivo + Los10), Tivozanib plus losartan (30 mg/kg; Tivo + Los30) or vehicle control. Protein expression of angiotensin-II type 1 (AT1) receptor in the aorta.

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    Description

    Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy[1].

    IC50 & Target

    VEGFR2

    6.5 nM (IC50)

    VEGFR3

    15 nM (IC50)

    VEGFR1

    30 nM (IC50)

    In Vitro

    Tivozanib hydrate inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3, with IC50s of 0.16-0.24 nM[1].
    Tivozanib hydrate (0-100 nM, 24 h) inhibits VEGF-induced proliferation of HUVECs with IC50 of 0.67 nM, and migration of HUVECs in dose-dependent manner[1].
    Tivozanib hydrate (0-300 nM, 1 h) selectively inhibits the VEGF-stimulated phosphorylation of MAPKs in endothelial cells ligand-dependently, with IC50s of 0.13 and 0.18 nM for ERK1 and ERK2, respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Proliferation Assay[1]

    Cell Line: HUVECs
    Concentration: 0-100 nM
    Incubation Time: 24 h
    Result: Inhibited proliferation.

    Cell Migration Assay [1]

    Cell Line: HUVECs
    Concentration: 0-100 nM
    Incubation Time: 22 h
    Result: Inhibited migration.

    Western Blot Analysis[1]

    Cell Line: HUVECs
    Concentration: 0-300 nM
    Incubation Time: 1 h
    Result: Inhibited VEGR-dependent phosphorylation of ERK1 and ERK2.
    In Vivo

    Tivozanib hydrate (0.04-1 mg/kg, po for 14 days) exhibits antitumor efficacy against breast, colon,hepatic, lung, ovarian, pancreatic, and prostate cancer in model[1].
    Tivozanib hydrate (0.2-1 mg/kg, po for 21 days) reversibly suppresses vascular permeability and angiogenesis in Calu-6 tumor bearing rats model[1].
    Tivozanib hydrate (5 mg/kg, po, single dose) reveals a AUCinf of 44.5 μg·h/mL, Cmax of 2823 ng/mL in athymic mice model[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Calu-6 tumor bearing athymic mice model[1]
    Dosage: 0.04-1 mg/kg/day
    Administration: p.o., for 14-21 days
    Result: Inhibited tumor growth, angiogenesis and vascular permeability.
    Molecular Weight

    472.88

    Formula

    C22H21ClN4O6

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=C(C=C1Cl)OC2=CC=NC3=CC(OC)=C(C=C23)OC)NC4=NOC(C)=C4.O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMF : 30 mg/mL (63.44 mM; Need ultrasonic and warming)

    DMF : 30 mg/mL (63.44 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1147 mL 10.5735 mL 21.1470 mL
    5 mM 0.4229 mL 2.1147 mL 4.2294 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.0%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMF / DMF 1 mM 2.1147 mL 10.5735 mL 21.1470 mL 52.8675 mL
    5 mM 0.4229 mL 2.1147 mL 4.2294 mL 10.5735 mL
    10 mM 0.2115 mL 1.0574 mL 2.1147 mL 5.2868 mL
    15 mM 0.1410 mL 0.7049 mL 1.4098 mL 3.5245 mL
    20 mM 0.1057 mL 0.5287 mL 1.0574 mL 2.6434 mL
    25 mM 0.0846 mL 0.4229 mL 0.8459 mL 2.1147 mL
    30 mM 0.0705 mL 0.3525 mL 0.7049 mL 1.7623 mL
    40 mM 0.0529 mL 0.2643 mL 0.5287 mL 1.3217 mL
    50 mM 0.0423 mL 0.2115 mL 0.4229 mL 1.0574 mL
    60 mM 0.0352 mL 0.1762 mL 0.3525 mL 0.8811 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Tivozanib hydrate
    Cat. No.:
    HY-112467
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