溶解性 | Soluble in DMSO (~20 mg/ml), Hot Methanol, DMF (~20 mg/ml), 1:2 solution of DMSO:PBS(PH 7.2 ) (~0.3 mg/ml), 100% ethanol, and ethyl acetate. |
存贮条件 | 储存温度-20°C |
产品介绍 | Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂,IC50分别为6 nM, 22 nM和90 nM。还能抑制野生型和V599E突变型BRAF活性。 |
别名 | Nexavar;Bay 43-9006;索拉非尼; 4-{4-[3-(4-氯-3-三氟甲基苯基)酰脲]苯氧基}吡啶-2-甲酰胺;Raf抑制剂;4-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide;BAY 43-9006 |
生化机理 | Sorafenib is a RAF kinase inhibitor which suppresses ERK phosphorylation. Studies indicate that sorafenib induces c-Raf phosphorylation at both Ser-43 and Ser-259. When combined with vitamin K1, phosphorylation is increased at these serine residues. Sorafenib also induces the phosphorylation of PKA. In addition, sorafenib induces c-Met phosphorylation at Tyr-1349, which consequently induces PI3K-Akt phosphorylation. Studies determined that sorafenib inhibits other kinases such as Flk-1 (VEGFR2), PDGFR (platelet-derived growth factor receptor), Flt-3/Flk-2 (FLT3), Ret, and c-Kit. Sorafenib is an inhibitor of Raf-1, Raf-B, PDGFR-βand Flt-4. Its ability to affect the Raf/Mek/Erk pathway makes it useful in cancer research studies. |
应用 | An inhibitor of tyrosine protein kinases that targets the Raf/Mek/Erk pathway |
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