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Beschreibung

A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110alpha-selective PI3-K inhibitor (IC50 = 0.3, 40, 100, and 850 nM for p110alpha, p110gamma, PI 3-K C2beta, and p110beta, respectively). Shown to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC50 <=58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).