cyh-33 methanesulfonate

CYH33 methanesulfonate is a highly selective and orally active inhibitor of PI3Kα, with IC50 values of 5.9 nM, 598 nM, 78.7 nM, and 225 nM against the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits the phosphorylation of Akt and ERK, leading to a significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Additionally, CYH33 methanesulfonate demonstrates potent activity against solid tumors.

CYH33, an orally active and highly selective PI3Kα inhibitor, demonstrates specificity with IC50 values of 5.9 nM for the α isoform, 598 nM for β, 78.7 nM for δ, and 225 nM for γ. It effectively inhibits Akt and ERK phosphorylation and induces substantial G1 phase arrest in breast cancer and non-small cell lung cancer (NSCLC) cells, showcasing potent activity against solid tumors.