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

Tivozanib  (Synonyms: AV-951; KRN951)

Cat. No.: HY-10977 Purity: 99.37%
COA Handling Instructions

Tivozanib (AV-951; KRN951) is a selective and orally active VEGFR tyrosine kinase inhibitor with IC50 of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib has the potential for the research of metastatic renal cell carcinoma (RCC) .

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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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 95 In-stock
50 mg USD 317 In-stock
100 mg USD 554 In-stock
200 mg USD 990 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Tivozanib:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tivozanib (AV-951; KRN951) is a selective and orally active VEGFR tyrosine kinase inhibitor with IC50 of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib has the potential for the research of metastatic renal cell carcinoma (RCC) [1][2][3].

IC50 & Target[1]

VEGFR1

0.21 nM (IC50)

VEGFR2

0.16 nM (IC50)

VEGFR3

0.24 nM (IC50)

In Vitro

Tivozanib inhibits the phosphorylation of VEGFR-1, VEGFR-2 and VEGFR-3[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tivozanib (1 mg/kg; p.o.; 14 days) suppresses the development of CNV lesions and leds to a significant regression of established CNV, reducing the affected areas by 67.7%[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

  • Molarity Calculator

  • Dilution Calculator

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
Kinase Assay

Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of KRN951 against a variety of recombinant receptor and nonreceptor tyrosine kinases[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cell-based assays are done to determine the ability of KRN951 to inhibit ligand-dependent phosphorylation of receptor tyrosine kinases. Briefly, the cells are starved overnight in appropriate basic medium containing 0.5% fetal bovine serum (FBS). Following the addition of KRN951 or 0.1% DMSO, the cells are incubated for 1 hour and then stimulated with the cognate ligand at 37°C. Receptor phosphorylation is induced for 5 minutes except for VEGFR3 (10 minutes), c-Met (10 minutes), and c-Kit (15 minutes). All the ligands used in the assays are human recombinant proteins, except for VEGF-C, a rat recombinant protein. Following cell lysis, receptors are immunoprecipitated with appropriate antibodies and subjected to immunoblotting with phosphotyrosine. Quantification of the blots and calculation of IC50 values are carried out[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Cancer cells are s.c. inoculated into the right flank of the athymic rats. Once established, tumors of 1,500 mm3 are surgically excised and smaller tumor fragments (20-30 mg) are s.c. implanted in the right flank of irradiated rats. Oral administration of KRN951 (0.2 or 1 mg/kg) or vehicle is initiated at the day of randomization (day 0). Tumor volume is measured twice weekly with Vernier calipers, and calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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Tivozanib
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