BAG 956 is a dual PDK1 and class I PI 3-kinase inhibitor (IC50 values are 245, 56, 446, 35 and 117 nM for PDK1 and PI3K p110 -α, -β, -δ, and -γ respectively). BAG 956 has been shown to inhibit cellular AKT phosphorylation at Thr308. BAG 956 also blocks cell proliferation and causes arrest in the G1 phase of the cell cycle. BAG 956 has been shown to slow tumor progression in mouse xenograft models.
Stauffer et al (2008) Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg.Med.Chem.Lett. 18 1027. Weisberg et al (2008) Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells. Blood 111 3723. Marone et al (2009) Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol.Cancer Res. 7 601.
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