BAG 956

• Supplier: Tocris Bioscience
• Catalog: 1334
• Prices: $235.00, $965.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 853910-02-8
• Chemical Name: α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
• Formula: C28H21N5
• Molecular Weight: 427.5
• Purity: >99 %
• Description: Dual PDPK1 (PDK1) and class I PI 3-K inhibitor (IC 50 values are 245, 56, 446, 35 and 117 nM for PDPK1 and PI 3-K p110 - α , - β , - δ , and - γ respectively). Inhibits cellular AKT phosphorylation at Thr308. Blocks cell proliferation, causing arrest in G 1 phase of the cell cycle. Slows tumor progression in mouse xenograft models.

Product References

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. - Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

Stauffer F, Maira SM, Furet P, Garcia-Echeverria C. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1027-30.

Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: - Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956:

Weisberg E, Banerji L, Wright RD, Barrett R, Ray A, Moreno D, Catley L, Jiang J, Hall-Meyers E, Sauveur-Michel M, Stone R, Galinsky I, Fox E, Kung AL, Griffin JD. Blood. 2008 Apr 1;111(7):3723-34.

Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of - Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of

Marone R, Erhart D, Mertz AC, Bohnacker T, Schnell C, Cmiljanovic V, Stauffer F, Garcia-Echeverria C, Giese B, Maira SM, Wymann MP. Mol Cancer Res. 2009 Apr;7(4):601-13.