ST-168

ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement in MEK1 inhibition respectively, as compared to a previous lead ST-162 in in vitro enzymatic inhibition assays. ST-168 demonstrated superior tumoricidal efficacy over ST-162 in an A375 melanoma spheroid tumor model.