ST-162 is a potent, bifunctional MAPK/PI3K antagonist with IC50 of 191 nM and 398 nM for PI3Kα and MEK1, respectively.
ST-162 produces regression of mutant KRAS or BRAF addicted xenograft models of colorectal cancer and melanoma and stasis of BRAF/PTEN mutant melanomas.
ST-162 increases efficacy in a syngeneic KRAS mutant colorectal cancer model combined with checkpoint blocker PD-L1.
