| 应用 |
An inhibitor of tyrosine protein kinases that targets the Raf/Mek/Erk pathway |
| 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。
This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia. |
| 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. |
| 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 |
