ST-162

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

References 1. Galbán S, et al. Mol Cancer Ther. 2017 Nov;16(11):2340-2350. 2. Van Dort ME, et al. J Med Chem. 2016 Mar 24;59(6):2512-22. 3. Van Dort ME, et al. ACS Med Chem Lett. 2017 Jul 24;8(8):808-813. View Related Products by Target PI3K