R&D Systems Inc. Tocris Bioscience Boston Biochem

BAG 956

Cat. No. 3606

BAG 956 C28H21N5 [853910-02-8]

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Chemical Name: α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile

Biological Activity

Dual PDK1 and class I PI 3-K inhibitor (IC50 values are 245, 56, 446, 35 and 117 nM for PDK1 and PI 3-K p110 -α, -β, -δ, and -γ respectively). Inhibits cellular AKT phosphorylation at Thr308. Blocks cell proliferation, causing arrest in G1 phase of the cell cycle. Slows tumor progression in mouse xenograft models.

Technical Data

M.Wt:
427.5
Formula:
C28H21N5
Solubility:
Soluble to 40 mM in DMSO and to 20 mM in ethanol
Purity:
>99 %
Storage:
Store at RT
CAS No:
853910-02-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

Stauffer et al (2008) Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg.Med.Chem.Lett. 18 1027. PMID: 18248814.

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. PMID: 18184863.

Marone et al (2009) Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol.Cancer Res. 7 601. PMID: 19372588.

If you know of a relevant citation for this product please let us know.

Keywords: BAG 956, supplier, Dual, inhibitors, PDK, PDK1, PI3K, p110, inhibits, PI, 3-kinases, Signaling, Signalling, Phosphoinositide, Kinases, PIP2, Inositol, Lipids, cAMP, 3-phosphoinositide, dependent, protein, kinase-1, BAG956

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