ST-168

ST-168 is an orally bioavailable inhibitor of MEK and PI3K, exhibiting IC50 values of 182 nM for MEK1 and showing varying potency against PI3K isoforms with values of 69.2 nM, 41.7 nM, 1482 nM, and 2293 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively. It effectively inhibits ERK1/2 and AKT phosphorylation, inducing apoptosis in cancer cells within a 3D tumor sphere model. In vivo studies demonstrate its substantial antitumor efficacy in A375 melanoma mouse models. Additionally, ST-168 displays an improved ocular safety profile compared to conventional MEK inhibitors, evidenced by reduced caspase activation and apoptosis levels, making it a valuable tool for melanoma research.