| Name | Tivozanib |
| 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. |
| 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) |
| 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. |
| In vitro | In endothelial cells (IC 50 = 0.16 nM), Tivozanib was able to inhibit VEGF-induced phosphorylation of VEGFR2 |
| In vivo | In endothelial cells (IC 50 = 0.16 nM), Tivozanib was able to inhibit VEGF-induced phosphorylation of VEGFR2 |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.4 mM), Sonication is recommended.
DMSO : 38.33 mg/mL (84.27 mM), Sonication is recommended.
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| Keywords | VEGFR3 | VEGFR2 | VEGFR1 | VEGFR | vascular permeability | Vascular endothelial growth factor receptor | Tivozanib | renal cell carcinoma | PDGFRα | orally active | KRN-951 | KRN 951 | Inhibitor | inhibit | EphrinReceptor | Ephrin Receptor | EphB2 | AV951 | AV 951 | antitumor | angiogenesis |
| Inhibitors Related | Ribociclib | Regorafenib monohydrate | Sorafenib | glycine | Nintedanib esylate | Regorafenib | Ethyl cinnamate | Chloramphenicol | Thymoquinone | Lenvatinib | Pazopanib | Albendazole |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
