维罗非尼

  • 化学数据
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
  • 用途
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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