2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Tivozanib

Tivozanib  (Synonyms: AV-951; KRN951)

Cat. No.: HY-10977 Purity: 99.37%
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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.

Tivozanib Chemical Structure

Tivozanib Chemical Structure

CAS No. : 475108-18-0

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10 mM * 1 mL in DMSO
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Based on 6 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

VEGFR2

6.5 nM (IC50)

VEGFR3

15 nM (IC50)

VEGFR1

30 nM (IC50)

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.

Tivozanib Related Antibodies

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 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.
Clinical Trial
Molecular Weight

454.86

Formula

C22H19ClN4O5
CAS No.
Appearance

Solid

Color

Light brown to 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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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)

g

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
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, 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 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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