| product Name | Regorafenib hydrate |
|---|---|
| Synonyms | Regorafenib monohydrate |
| CAS Registry Number | 1019206-88-2 |
| Description | Regorafenib monohydrate (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor with potent anti-tumour and anti-angiogenic activity. It is approved for the treatment of metastatic colorectal cancer, advanced gastrointestinal mesenchymal stromal tumours and hepatocellular carcinoma. |
| Uses | 4-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide Hydrate can be used as an anti-tumor drug. |
| Biological Activity | regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with ic50 values of 13nm, 4.2nm, 46nm, 2.5nm, 28nm, 19nm, 202nm, 22nm, 7nm, 1.5nm and 311nm, respectively for vegfr-1, mvegfr-2, mvegfr-3, raf-1, braf wt, brafv600e, fgfr-1, pdgfr-β, c-kit, retand tie2 [1].regorafenib is a multikinase inhibitor of both intracellular and membrane-bound rtks. it shows potent inhibition of angiogenic and stromal rtks like vegf receptors-1-3, pdgfr-β and fgf receptor-1 with ic50 values ranging from4.2 to 311nm in biochemical assays. it also inhibits oncogenic rtks, such as ret and c-kit, with ic50 values ranging from 1.5 to 28nm in cellular assays [1].regorafenib is reported to have anti-tumor efficacy to various tumors including breast, pancreas, thyroid, melanoma, gist, and crc with a mean ic50 value less than 1μm. these inhibition effects of tumor growth are also found in mouse xenograft models after the treatment of regorafenib at dose ranging from 10 to 100 mg/kg [1]. |
| Mechanism of action | The mechanism of anticancer action of Regorafenib monohydrate is similar to that of Regorafenib, an oral multikinase inhibitor that blocks tyrosine kinases that are active in angiogenesis, cancer development and growth, and maintenance of the tumour microenvironment. It is superior to sorafenib in blocking both vascular endothelial growth factor receptor and TIE2, a molecule with an important role in angiogenesis. |
| Raw materials | Regorafenib |
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