rmc-4550

Description: RMC-4550 is a novel, potent, selective and allosteric inhibitor of SHP2 phosphatase with an IC50 of 0.583 nM. RMC-4550 is a potent and selective SHP2 inhibitor. RMC-4550 identified as a high quality tool compound to study the role of SHP2 in tumor biology, both in vitro and in vivo in rodents. SHP2 is a convergent signalling node and inhibition of SHP2 is effective in targeting both upstream (RTK-driven) and downstream (RAS-GTP dependent) mutations in the RAS-MAPK pathway. Oncogenic alterations in the RAS/RAF/MEK/ERK pathway drive the growth of a wide spectrum of cancers. While BRAF and MEK inhibitors are efficacious against BRAFV600E-driven cancers, effective targeted therapies are lacking for most cancers driven by other pathway alterations, including non-V600E oncogenic BRAF, RAS GTPase-activating protein (GAP) NF1 (neurofibromin 1) loss and oncogenic KRAS.

References: Nat Cell Biol. 2018 Sep; 20(9):1064-1073.