RMC4550

  • Chemical Properties
CAS No. 2172651-73-7 Cat. No. BCP30530
Name RMC4550
Synonyms RMC 4550; RMC4550;
Formula C21H26Cl2N4O2 M. Wt 437.36
  • Biological Activity
Description 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.
Pathways Protease/Metabolic Enzyme 
Targets Phosphatase 

Structure

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