AV-951 is an potent and selective orally bioavailable isoxazole inhibitor of VEGFR1, 2, and 3, kinases at 0.21, 0.16, and 0.24 nM, respectively. Additionally it has nanomolar activity for cKIT and PDGFR at 1.63 and 1.72 nM, respectively. [1] In vitro, AV-951 blocks MAP kinase activation and suppresses the proliferation and migration of endothelial cells. In vivo, it suppresses angiogenesis and tumor progression in human xenografts. [2]AV-951 has been widely studied in clinical trials for the treatment of advanced renal cell carcinoma (RCC) and non-small cell lung cancers (NSCLC). More recent studies are exploring combination therapies with paclitaxel and bevacizumab for breast and colorectal cancer, respectively.
Technical information:
| Chemical Formula: | C22H19ClN4O5 | |
| CAS #: | 475108-18-0 | |
| Molecular Weight: | 454.86 | |
| Purity: | > 98% | |
| Appearance: | Off White | |
| Chemical Name: | 1-(2-chloro-4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-3-(5-methylisoxazol-3-yl)urea | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AV-951, AV 951, AV951, Tivozanib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Eskens et al., Biologic and clinical activity of tivozanib (AV-951, KRN-951), a selective inhibitor of VEGF receptor-1, -2, and -3 tyrosine kinases, in a 4-week-on, 2-week-off schedule in patients with advanced solid tumors. Clin Cancer Res 2011, 17, 7156-7163 Pubmed ID:21976547 |
| 2. | Campas et al., Tivozanib. Drugs Fut 2009, 34 (10), 793 Pubmed ID:ISSN: 0377-8282 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
