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Regorafenib is an orally bioavailable multikinase inhibitor. This compound is clinically used in the treatment of metastatic colorectal cancer and non-responsive gastrointestinal stromal tumors. Regorafenib displays anticancer chemotherapeutic and anti-angiogenic properties, selective primarily for VEGFR2 but also displaying inhibitory activity against TIE2, VEGFR1/3, PDGFR-β, FGFR1, c-Kit, RET, and B-Raf.
| Cas No. | 1019206-88-2 |
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| Purity | ≥99% |
| Formula | C21H15ClF4N4O3 • H2O |
| Formula Wt. | 500.83 |
| IUPAC Name | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3- fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrate |
| Synonym | BAY73-4506 |
| Solubility | insoluble in water between pH1 and 13, slightly soluble in methanol; ethanol and sparingly soluble in acetone |
| Appearance | off-white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet | |
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Abou-Elkacem L, Arns S, Brix G, et al. Regorafenib inhibits growth, angiogenesis, and metastasis in a highly aggressive, orthotopic colon cancer model. Mol Cancer Ther. 2013 Jul;12(7):1322-31. PMID: 23619301.
Wilhelm SM, Dumas J, Adnane L, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011 Jul 1;129(1):245-55. PMID: 21170960.