Cat. No.: HY-10977A

Tivozanib hydrochloride hydrate

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

10 Cited Publications

Customer Review

Based on 10 publication(s) in Google Scholar

Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride 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 hydrochloride hydrate exhibits antitumor efficacy.

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

Purity: 99.83%
CAS No.: 682745-41-1
Formula: C₂₂H₂₂Cl₂N₄O₆
Molecular Weight:509.34

Storage:

4°C, sealed storage, away from moisture and light

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

Tivozanib hydrochloride hydrate Chemical Structure

CAS No.: 682745-41-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[3]

VEGFR-2

6.5 nM (IC₅₀)

VEGFR-3

15 nM (IC₅₀)

VEGFR-1

30 nM (IC₅₀)

All VEGFR Isoforms :

In Vitro

Tivozanib hydrochloride hydrate inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3, with IC₅₀s of 0.16-0.24 nM^[1].
Tivozanib hydrochloride 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 hydrochloride 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 hydrochloride hydrate (0.04-1 mg/kg, po for 14 days) exhibits antitumor efficacy against breast, colon, hepatic, lung, ovarian, pancreatic, and prostate cancer in athymic mice model^[1].
Tivozanib hydrochloride 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 hydrochloride hydrate (5 mg/kg, po, single dose) reveals a AUC_inf of 44.5 μg·h/mL, C_max 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.

Chemical Information

CAS No. 682745-41-1
Appearance Solid
Molecular Weight 509.34
Formula C₂₂H₂₂Cl₂N₄O₆
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.Cl.O
Synonyms

AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Publications (10)

All WBIn Vivo Efficacy StudyHistological Imaging/Staining

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Journal Impact Factor

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 hydrochloride 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 hydrochloride 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.
Cell Mol Gastroenterol Hepatol

Sorafenib Promotes Treg Cell Differentiation To Compromise Its Efficacy via VEGFR/AKT/Foxo1 Signaling in Hepatocellular Carcinoma. [Abstract]

2025;19(5):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 hydrochloride 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 hydrochloride 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 hydrochloride 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.
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
Res Sq

2026 May 20.
SSRN

2026 May 20.
Technical University of Munich

24.01.2018.
Patent

US20170349880A1.

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (245.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9633 mL

9.8166 mL

19.6333 mL

5 mM

0.3927 mL

1.9633 mL

3.9267 mL

10 mM

0.1963 mL

0.9817 mL

1.9633 mL

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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Nakamura K, et al., KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res. 2006 Sep 15;66(18):9134-42. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9633 mL	9.8166 mL	19.6333 mL	49.0831 mL
	5 mM	0.3927 mL	1.9633 mL	3.9267 mL	9.8166 mL
	10 mM	0.1963 mL	0.9817 mL	1.9633 mL	4.9083 mL
	15 mM	0.1309 mL	0.6544 mL	1.3089 mL	3.2722 mL
	20 mM	0.0982 mL	0.4908 mL	0.9817 mL	2.4542 mL
	25 mM	0.0785 mL	0.3927 mL	0.7853 mL	1.9633 mL
	30 mM	0.0654 mL	0.3272 mL	0.6544 mL	1.6361 mL
	40 mM	0.0491 mL	0.2454 mL	0.4908 mL	1.2271 mL
	50 mM	0.0393 mL	0.1963 mL	0.3927 mL	0.9817 mL
	60 mM	0.0327 mL	0.1636 mL	0.3272 mL	0.8181 mL
	80 mM	0.0245 mL	0.1227 mL	0.2454 mL	0.6135 mL
	100 mM	0.0196 mL	0.0982 mL	0.1963 mL	0.4908 mL

Keywords

Tivozanib hydrochloride hydrate

10 Cited Publications

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Tivozanib hydrochloride hydrate

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Publications Citing Use of MedChemExpress (MCE) Tivozanib hydrochloride hydrate

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tivozanib hydrochloride hydrate Related Classifications

HY-10977A Related Classifications