Tivozanib

SKU: orb1305458

Description

Tivozanib (KRN951) is an orally active small molecule inhibitor targeting VEGFR-1, -2, and -3. It exhibits potent antiangiogenic activity and is widely used in preclinical oncology research, including in vitro kinase assays and in vivo xenograft models for various solid tumors.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 475108-18-0
• MW: 454.86
• Purity: 99.67% (May vary between batches)
• Formula: C₂₂H₁₉ClN₄O₅
• SMILES: O(C=1C2=C(C=C(OC)C(OC)=C2)N=CC1)C3=CC(Cl)=C(NC(NC=4C=C(C)ON4)=O)C=C3
• Target: Ephrin Receptor,VEGFR,PDGFR
• Solubility: DMSO:38.33 mg/mL (84.27 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.4 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PDGFRα:40 nM|VEGFR2:6.5 nM|VEGFR3:15 nM|EphB2:24 nM|VEGFR1:30 nM
• In Vivo:
  In endothelial cells (IC 50 = 0.16 nM), Tivozanib was able to inhibit VEGF-induced phosphorylation of VEGFR2
• In Vitro:
  In endothelial cells (IC 50 = 0.16 nM), Tivozanib was able to inhibit VEGF-induced phosphorylation of VEGFR2
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

angiogenesis, antitumor, AV 951, AV951, AV-951, Inhibitor, EphB2, Ephrin Receptor, EphrinReceptor, inhibit, KRN 951, KRN951, KRN-951, orally active, VEGFR2, VEGFR1, VEGFR, VEGFR3, vascular permeability, Vascular endothelial growth factor receptor, PDGFRα, Tivozanib, renal cell carcinoma

Compound Identifiers

PubChem CID

9911830