塞尔帕替尼

  • 化学数据
CAS号 2152628-33-4 货号 BCP29047
中文名 塞尔帕替尼
英文名 Selpercatinib
中文别名 塞卡替尼;
英文别名 LOXO-292;LOXO 292;LOXO292;
分子式 C29H31N7O3 分子量 525.25
  • 用途
生物活性 Selpercatinib is an orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, selpercatinib selectively binds to and targets wild-type RET as well as various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. In addition, selpercatinib targets, binds to and inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and 3 (VEGFR3), and fibroblast growth factor receptor 1 (FGFR1), 2 (FGFR2), and 3 (FGFR3). RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.
信号通路 Angiogenesis/Protein Tyrosine Kinase 
靶 点 RET 

结构式

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