RMC-4550

  • 化学数据
CAS号 2172651-73-7 货号 BCP30530
中文名 RMC-4550
英文名 RMC4550
中文别名
英文别名 RMC 4550; RMC4550;
分子式 C21H26Cl2N4O2 分子量 437.36
  • 用途
生物活性 RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM; shows no activity against the SHP2 catalytic domain up to 10 uM, RMC-4550 is highly selective for full-length SHP2 across panels comprising 15 other phosphatases, 468 kinases, and 44 cellular targets; cancer cell lines bearing missense mutations in KRAS at G12, but neither G13 nor Q61, exhibit sensitivity to RMC-4550 (IC50<2 uM), suppresses growth and RAS/MAPK signaling in cancer cell lines with Class 3 BRAF mutations; inhibits tumor growth and RAS/MAPK signaling in xenograft models of KRASG12C-driven cancer.
信号通路 Protease/Metabolic Enzyme 
靶 点 Phosphatase 

结构式

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