RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction[1].
RMC-0331 has an IC50 of 71 nM measuring by the rate of GDP/GTP exchange in vitro[1].
RMC-0331 (100-250 mg/kg; p.o.; qd; immunocompetent mice) shows single agent anti-tumor activity in SHP2-mutant models[1].
[1]. Andreas Buckl, et al. Discovery of a Potent, Selective and Orally Bioavailable SOS1 Inhibitor, RMC-0331 (RM-023), an in vivo Tool Compound that Blocks RAS Activation via Disruption of the RAS-SOS1 Interaction.