Cat. No.: HY-10977

Tivozanib

(Synonyms: AV-951; KRN951)

10 Cited Publications

Customer Review

Based on 10 publication(s) in Google Scholar

Tivozanib (AV-951; KRN951) 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 exhibits antitumor efficacy.

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

Purity: 99.80%
CAS No.: 475108-18-0
Formula: C₂₂H₁₉ClN₄O₅
Molecular Weight:454.86

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tivozanib Chemical Structure

CAS No.: 475108-18-0

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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
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (10)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

VEGFR2

6.5 nM (IC₅₀)

VEGFR3

15 nM (IC₅₀)

VEGFR1

30 nM (IC₅₀)

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.62 μM Compound: Tivozanib	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37453330]
B16-F10	IC₅₀	18.8 μM Compound: 10	Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38870832]
HUVEC	IC₅₀	>300 nM Compound: Chemical probe: KRN951	Antiproliferative activity against bFGF-induced human HUVEC cells assessed as cell viability incubated for 72 hrs by WST-1 assay Antiproliferative activity against bFGF-induced human HUVEC cells assessed as cell viability incubated for 72 hrs by WST-1 assay	[PMID: 16982756]
HUVEC	IC₅₀	0.67 nM Compound: Chemical probe: KRN951	Antiproliferative activity against VEGF-induced human HUVEC cells assessed as cell viability incubated for 72 hrs by WST-1 assay Antiproliferative activity against VEGF-induced human HUVEC cells assessed as cell viability incubated for 72 hrs by WST-1 assay	[PMID: 16982756]
Macrophage	IC₅₀	226.75 μM Compound: Tivozanib	Cytotoxicity against human Primary macrophage cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Cytotoxicity against human Primary macrophage cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37453330]
MCF7	IC₅₀	0.38 μM Compound: Tivozanib	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 24583357]
MCF7	IC₅₀	0.38 μM Compound: Tivozanib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37453330]
NCI-H460	IC₅₀	0.39 μM Compound: Tivozanib	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 37453330]

In Vitro

Tivozanib inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3, with IC₅₀s of 0.16-0.24 nM^[1].
Tivozanib (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 (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.

Western Blot Analysis^[1]

Cell Line:

HUVECs
Concentration:

0-300 nM
Incubation Time:

1 h
Result:

Inhibited VEGR-dependent phosphorylation of ERK1 and ERK2.

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.

In Vivo

Tivozanib (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 (0.2-1 mg/kg, po for 21 days) reversibly suppresses vascular permeability and angiogenesis in Calu-6 tumor bearing rats model^[1].
Tivozanib (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 475108-18-0
Appearance Solid
Molecular Weight 454.86
Formula C₂₂H₁₉ClN₄O₅
Color Off-white to light brown
SMILES

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

AV-951; KRN951
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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 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 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 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 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 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 : 25 mg/mL (54.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.1985 mL

10.9924 mL

21.9848 mL

5 mM

0.4397 mL

2.1985 mL

4.3970 mL

10 mM

0.2198 mL

1.0992 mL

2.1985 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1985 mL	10.9924 mL	21.9848 mL	54.9620 mL
	5 mM	0.4397 mL	2.1985 mL	4.3970 mL	10.9924 mL
	10 mM	0.2198 mL	1.0992 mL	2.1985 mL	5.4962 mL
	15 mM	0.1466 mL	0.7328 mL	1.4657 mL	3.6641 mL
	20 mM	0.1099 mL	0.5496 mL	1.0992 mL	2.7481 mL
	25 mM	0.0879 mL	0.4397 mL	0.8794 mL	2.1985 mL
	30 mM	0.0733 mL	0.3664 mL	0.7328 mL	1.8321 mL
	40 mM	0.0550 mL	0.2748 mL	0.5496 mL	1.3740 mL
	50 mM	0.0440 mL	0.2198 mL	0.4397 mL	1.0992 mL

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Tivozanib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) Tivozanib

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (10)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tivozanib Related Classifications

HY-10977 Related Classifications