SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising drug candidate for the research of KRAS-driven cancer.In Vitro:SOS1-IN-15 (Compound 37) (0.1 nM-0.1 mM; 72 h) displays prominent inhibitory activities in Mia-paca-2 cancer cells (IC50 = 178 ± 42 nM).
SOS1-IN-15 has a limited inhibition of CYP and hERG.In Vivo:SOS1-IN-15 (Compound 37) (50 mg/kg; p.o.; daily for 22 days) inhibits tumor volume in mice.