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.

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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