Tivozanib (Synonyms: AV-951; KRN951)

Name: Tivozanib
Brand: MedChemExpress
SKU: HY-10977
Rating: 5.0 (8 reviews)

Cat. No.: HY-10977 Purity: 99.80%: Data Sheet
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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.

CAS No. : 475108-18-0

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Tivozanib:

Tivozanib hydrochloride hydrate In-stock
Tivozanib hydrate In-stock
Tivozanib-d₆ Get quote
Tivozanib (Standard) Get quote

8 Publications Citing Use of MCE Tivozanib

In Vivo Efficacy Study

Histological Imaging/Staining

: 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.

: Tivozanib 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 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 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

VEGFR2

6.5 nM (IC₅₀)

VEGFR3

15 nM (IC₅₀)

VEGFR1

30 nM (IC₅₀)

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	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]
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]
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]
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]
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

Molecular Weight

454.86

Formula

C₂₂H₁₉ClN₄O₅

CAS No.

475108-18-0

Appearance

Solid

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (255 KB) HNMR (277 KB) RP-HPLC (244 KB) LCMS (100 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]

Complete Stock Solution Preparation Table

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

Tivozanib Related Classifications

Help & FAQs

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.

Keywords:

Tivozanib475108-18-0AV-951 KRN951AV951AV 951KRN951KRN 951KRN-951VEGFRVascular endothelial growth factor receptororally activeangiogenesisvascular permeabilityantitumorrenal cell carcinomaInhibitorinhibitorinhibit

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Tivozanib (Synonyms: AV-951; KRN951)

Customer Review

Other Forms of Tivozanib:

Tivozanib Related Antibodies

8 Publications Citing Use of MCE Tivozanib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tivozanib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tivozanib Related Classifications

Keywords:

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Customer Review

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