Tivozanib hydrate
Based on 10 publication(s) in Google Scholar
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.
- Purity: 99.0%
- CAS No.: 682745-40-0
- Formula: C22H21ClN4O6
- Molecular Weight:472.88
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tivozanib hydrate
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Angiogenesis. 2025 Feb 3;28(2):13. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2024 Dec 30:101454. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Pharmaceuticals (Basel). 2023 Feb 14;16(2):295. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Res Sq. 2026 May 20.
- SSRN. 2026 May 20.
- Technical University of Munich. 24.01.2018.
- Patent. US20170349880A1.
Customer Validation & Images
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WB
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In Vivo Efficacy Study
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Histological Imaging/Staining
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All VEGFR Isoforms
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Biological Activity
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VEGFR2 6.5 nM (IC50) |
VEGFR3 15 nM (IC50) |
VEGFR1 30 nM (IC50) |
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.
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Cell Line:HUVECs
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Concentration:0-100 nM
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Incubation Time:24 h
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Result:Inhibited proliferation.
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Cell Line:HUVECs
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Concentration:0-100 nM
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Incubation Time:22 h
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Result:Inhibited migration.
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Cell Line:HUVECs
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Concentration:0-300 nM
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Incubation Time:1 h
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Result:Inhibited VEGR-dependent phosphorylation of ERK1 and ERK2.
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.
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Animal Model:Calu-6 tumor bearing athymic mice model[1]
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Dosage:0.04-1 mg/kg/day
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Administration:p.o., for 14-21 days
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Result:Inhibited tumor growth, angiogenesis and vascular permeability.
Chemical Information
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CAS No. 682745-40-0
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Appearance Solid
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Molecular Weight 472.88
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Formula C22H21ClN4O6
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C=C1Cl)OC2=CC=NC3=CC(OC)=C(C=C23)OC)NC4=NOC(C)=C4.O
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Synonyms
AV-951 hydrate; KRN951 hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Angiogenesis
Clioquinol inhibits angiogenesis by promoting VEGFR2 degradation and synergizes with AKT inhibition to suppress triple-negative breast cancer vascularization. [Abstract]2025 Feb 3;28(2):13. PMID: 39899169
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.
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Cell Mol Gastroenterol Hepatol
Sorafenib Promotes Treg Cell Differentiation To Compromise Its Efficacy via VEGFR/AKT/Foxo1 Signaling in Hepatocellular Carcinoma. [Abstract]2024 Dec 30:101454. PMID: 39743020 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Pharmaceuticals (Basel)
Mechanism Underlying Triple VEGFR Inhibitor Tivozanib-Induced Hypertension in Mice Model. [Abstract]2023 Feb 14;16(2):295. PMID: 37259438
Tivozanib hydrate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2023 Feb 14;16(2):295. [Abstract]
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. [Abstract]
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. [Abstract]
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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PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
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Solvent & Solubility
DMF : 30 mg/mL (63.44 mM; Need ultrasonic and warming)
DMF : 30 mg/mL (63.44 mM; Need ultrasonic and warming)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 |
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| 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 |
Tivozanib hydrate Related Classifications
HY-112467 Related Classifications
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