维罗非尼
CAS号 | 1029872-54-5 | 货号 | BCP43160 |
中文名 | 维罗非尼 | ||
英文名 | Vemurafenib | ||
中文别名 | |||
英文别名 | PLX4032;PLX-4032;PLX 4032; | ||
分子式 | C23H18ClF2N3O3S | 分子量 | 489.92 |
生物活性 | Vemurafenib is an orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers. | ||
上下游产品 | 918504-65-1(维罗非尼) | ||
信号通路 | MAPK Pathway | ||
靶 点 | Raf |
结构式
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