GSK547

  • 化学数据
CAS号 2226735-55-1 货号 BCP30590
中文名 GSK547
英文名 GSK547
中文别名
英文别名 GSK-547; GSK 547; RIP1i;
分子式 C20H18F2N6O 分子量 396.40
  • 用途
生物活性 GSK547 (RIP1i, GSK 547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo; exhibited a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963; reprogrammed TAMs toward an MHCIIhiTNFα+IFNγ+ immunogenic phenotype in a STAT1-dependent manner. RIP1 inhibition in TAMs resulted in cytotoxic T cell activation and T helper cell differentiation toward a mixed Th1/Th17 phenotype, leading to tumor immunity in mice and in organotypic models of human Pancreatic ductal adenocarcinoma (PDA).
信号通路 Apoptosis Pathway 
靶 点 RIP 

结构式

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