MRTX0902 is a highly potent, selective SOS1 inhibitor with binding IC50 of 2 nM, cellular IC50 of 33 nM (pERK).
MRTX0902 displays weak to no affinity for SOS2 with IC50 of >10 uM.
MRTX0902 exhibits promising potency, selectivity, and exposure in preclinical species.
MRTX0902 in combined with MRTX849 demonstrates durable regression in KRasG12C NSCLC and CRC PDX models.
MRTX0902 demonstrates improved efficacy with osimertinib (EGFRi), VS-6766 (RAF/MEKc) in MAPK tumor models.
