Catalog Number: 3606
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 PDPK1 (PDK1) and class I PI 3-K inhibitor (IC50 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 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.
Background References
  1. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.
    Stauffer et al.
    Bioorg.Med.Chem.Lett., 2008;18:1027
  2. Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells.
    Weisberg et al.
    Blood, 2008;111:3723
  3. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors.
    Marone et al.
    Mol.Cancer Res., 2009;7:601

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