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 potent and 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 87 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 112 In-stock
Estimated Time of Arrival: December 31
50 mg USD 317 In-stock
Estimated Time of Arrival: December 31
100 mg USD 554 In-stock
Estimated Time of Arrival: December 31
200 mg USD 990 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Tivozanib:

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tivozanib (AV-951; KRN951) is a potent and 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].

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].

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.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (54.96 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tivozanib
Cat. No.:
HY-10977
Quantity:
MCE Japan Authorized Agent: