A-674563 (hydrochloride)

Uses

A-674563 Hydrochloride is a potent, orally available Akt1 inhibitor.

Biological Activity

A-674563 is an orally available ATP-competitive pan-AKT (PKB, protein Kinase B) inhibitor (AKT1 Ki = 11 nM) with additional potency against PKA, Cdk2 GSK3β (IC50 = 1.4, 4.2,10 nM, respectively). A-674563 reduces the phosphorylation of cellular Akt substrates (0.1-10 μM; MiaPaCa-2) and enhances paclitaxel efficacy in a PC-3 xenograft model in mice in vivo (40 mg A-674563/kg via p.o. b.i.d. for 21 days, 15 mg paclitaxel/day on days 20, 24, 28).