Methanone, [4-[[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]amino]-2-chloro-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidin-6-yl](tetrahydro-4-methoxy-2H-pyran-4-yl)-

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.