| product Name |
Sorafenib tosylate |
| Synonyms |
SORAFENIB-D3; 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide monomethanesulfonate; N-[4-Chloro-3-(trifluoromethyl)phenyl]-N’-[4-[2-(N-methylcarbamoyl)-4-pyridyloxy]phenyl]urea Tolsylate; Sorafenib TsOH salt |
| Molecular Formula |
C21H16ClF3N4O3・C7H8SO<s |
| Molecular Weight |
637.03 |
| CAS Registry Number |
475207-59-1;4750207-59-1 |
| Molecular Structure |
|
| Indications and Usage |
Sorafenib tosylate is a new type of multi-target antitumor drug, was developed by the German Bayer Pharmaceuticals, and displayed expansive antitumor activity in preclinical animal tests. Sorafenib tosylate is mainly used in advanced liver cancer treatment and is well tolerated. |
| Mechanisms of Action |
Sorafenib tosylate can simultaneously affect tumor cells and tumor blood vessels. It has a double antitumor effect: it can block the cell signal transduction pathways mediated by RAF/MEK/ERK to directly inhibit tumor cell growth, while also inhibiting VEGF and platelet derived growth factors (PDGF) receptors to prevent the formation of new tumor blood vessels, thus indirectly inhibiting tumor cell growth. |
| Description |
Sorafenib (475207-59-1) was initially developed as a Raf kinase inhibitor, IC50 = 6 nM, but has been shown to inhibit many receptor tyrosine kinases including BRAF (IC50 = 22 nM); VEGFR-2 (IC50 = 90 nM); VEGFR-3 (IC50 = 20 nM); PDGFR-β (IC50 = 57 nM); Flt3 (IC50 = 58 nM); c-KIT (IC50 = 68 nM); FGFR-1 (IC50 = 580 nM).1?Paradoxically more potent in a cellular assay (IC50 = 20 nM) compared to an isolated enzyme assay (IC50 = 107 nM) for c-Fms.2?Inhibits activation of MAPK pathway and ERK phosphorylation.3?Induces caspase-independent apoptosis in melanoma cells.4?Sorafenib is a clinically useful anticancer agent. |
| Uses |
Sorafenib Tosylate (Bay 43-9006, Nexavar) is a small molecular inhibitor of VEGFR, PDGFR, c-Raf and B-Raf with IC50s of 18 nM, 10 nM, 3 nM and 15 nM, respectively. |
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