Product Description
BAY-73-4506 (Regorafenib) is an orally active and highly potent inhibitor against multiple tyrosine kinases, including VEGFR1/2/3, PDGFR?, Kit, RET and Raf-1. Regorafenib inhibits the proliferation of HUVEC cells stimulated with VEGF, and inhibits FGFR signaling in breast cancer MCF-7 cells stimulated with FGF. Regorafenib is anti-angiogenic due to its inhibitions against VEGFR2-TIE2 tyrosine kinase. [1]Co-administration of Regorafenib and a PI3K/Akt inhibitor (MK-2206) clearly demonstrated synergistic effect in a HCT116 xenocraft mouse model [2]. Regorafenib is currently being studied as a potential treatment option in multiple tumor types, and has recently be approved in treating patients with Metastatic Colorectal cancer. [3]
Technical information:
| Chemical Formula: | C21H15ClF4N4O3 | |
| CAS #: | 755037-03-7 | |
| Molecular Weight: | 482.82 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | BAY-73-4506, BAY73-4506, Regorafenib, Fluoro-Sorafenib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Wilhelm SM et al, Regorafenib (BAY 73-4506): a new oral multi-kinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011; 129:245-55 Pubmed ID: 21170960 |
| 2. | Sajithlal GB et al. Sorafenib/regorafenib and phosphatidyl inositol 3 kinase/thymoma viral proto-oncogene inhibition interact to kill tumor cells. Mol Pharmacol. 2013; 84(4):562-71. Pubmed ID: 23877009 |
| 3. | Carter NJ. Regorafenib: a review of its use in previously treated patients with progressive metastatic colorectal cancer. Drugs Aging. 2014; 31(1):67-78. Pubmed ID: 24276917 |
