Doxecitine CAS# 951-77-9 2’-脱氧胞苷

Doxecitine (also known as SR-13668) is an orally bioavailable PI3K/Akt inhibitor. In vitro, it suppresses proliferation of a broad range of human tumor cell lines (colon, breast, prostate) with GI50 values typically in the low micromolar range (~0.5–5 µM depending on line) and induces caspase activation and apoptosis. It inhibits Akt phosphorylation and downstream survival signaling. In vivo, oral dosing in xenograft models (e.g., HCT-116 colon cancer or MCF-7 breast cancer) produced dose-dependent tumor growth suppression: ~40–70% tumor volume inhibition at well-tolerated daily oral doses in the 10–50 mg/kg range, with some studies reporting complete stasis at higher exposures. Oral bioavailability in rodents has been shown to be high because of limited first-pass metabolism. Overall, Doxecitine is a potent Akt pathway antagonist with demonstrated oral anticancer efficacy in preclinical models.