Capivasertib CAS# 1143532-39-1 (S)-4-氨基-N-(1-(4-氯苯基)-3-羟基丙基)-1-(7H-吡咯并[2,3-d]嘧啶-4-基)哌啶-4-羧酰胺

Capivasertib (AZD5363) is a potent, selective pan-AKT inhibitor with preclinical efficacy across multiple tumor models. It inhibited AKT1/2/3 with IC₅₀ values of 0.04–0.08 μM and suppressed downstream signaling by reducing phosphorylation of PRAS40 and GSK3β. In vitro, it inhibited proliferation of PI3K/PTEN-pathway–altered cancer cell lines with GI₅₀ values in the 0.1–0.5 μM range. In xenograft models, capivasertib demonstrated significant antitumor activity, achieving tumor regressions in PTEN-deficient and PIK3CA-mutant tumors at oral doses of 100–150 mg/kg. Combination with agents such as docetaxel or fulvestrant enhanced tumor growth inhibition, supporting its therapeutic potential in PI3K/AKT-driven cancers.