Afuresertib

1047644-62-1

C18H17Cl2FN4OS

DMSO : >= 40 mg/mL (93.61 mM)

PI3K/Akt/mTOR

Afuresertib is a potent and ATP-competitive specific Akt inhibitor. IC50 & Target: Akt^[1] In Vitro: Afuresertib exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G₁ phase. Western blotting analysis shows that Afuresertib increases the expression of p21^WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3beta and FOXO family proteins. Afuresertib-induced p21 expression promotes G₁ phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response^[1].