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Tivozanib

Catalog No. T2456   CAS 475108-18-0
Synonyms: AV-951, KRN951

Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

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Tivozanib Chemical Structure
Tivozanib, CAS 475108-18-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 76.00
25 mg In stock $ 145.00
50 mg In stock $ 252.00
100 mg In stock $ 450.00
200 mg In stock $ 663.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 98.23%
Purity: 97.41%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
Targets&IC50 PDGFRα:40 nM, EphB2:24 nM, VEGFR1:30 nM, VEGFR3:15 nM, VEGFR2:6.5 nM
Kinase Assay Kinase Assays: Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1.
Cell Research Human umbilical vein endothelial cells (HUVEC) and normal human dermal fibroblasts-based assays are done to determine the ability of AV-951 to inhibit ligand-dependent phosphorylation of tyrosine kinase receptors. The cells are starved overnight in appropriate basic medium containing 0.5% fetal bovine serum (FBS). The cells are incubated for 1 hour following the addition of AV-951 or 0.1% DMSO, 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 ou(Only for Reference)
Synonyms AV-951, KRN951
Molecular Weight 454.86
Formula C22H19ClN4O5
CAS No. 475108-18-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 16 mg/mL (35.2 mM)

TargetMolReferences and Literature

1. Nakamura K, et al. Cancer Res, 2006, 66(18), 9134-9142. 2. Taguchi E, et al. Cancer Sci, 2008, 99(3), 623-630.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Liver Cancer Compound Library Anti-Ovarian Cancer Compound Library Neural Regeneration Compound Library Inhibitor Library Anti-Obesity Compound Library

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Keywords

Tivozanib 475108-18-0 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Ephrin Receptor PDGFR antitumor vascular permeability renal cell carcinoma AV951 AV-951 angiogenesis AV 951 Inhibitor Vascular endothelial growth factor receptor KRN951 KRN 951 orally active inhibit KRN-951 inhibitor

 

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