BAG 956CAS: 853910-02-8
MF: C28H21N5
MW: 427.50
A dual PDK1 and class I PI 3-kinase inhibitor.

BAG 956 (CAS 853910-02-8)

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Synonym: 2-Methyl-2-[4-(2-methyl-8-pyridin-3-ylethynyl-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile
Application: A dual PDK1 and class I PI 3-kinase inhibitor
CAS Number: 853910-02-8
Purity: ≥99%
Molecular Weight: 427.50
Molecular Formula: C28H21N5
* Refer to Certificate of Analysis for lot specific data (including water content).

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.


References

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.

Physical State :
Solid
Solubility :
Soluble in DMSO (40 mM), and ethanol (20 mM).
Storage :
Store at room temperature
IC50 :
PDK1: IC50 = 245.56 nM; PI 3-K p110 -α: IC50 = 56 nM; PI 3-K p110 -β: IC50 = 446 nM; PI 3-K p110 -δ: IC50 = 35 nM; PI 3-K p110 -γ: IC50 = 117 nM; VEGFR1: IC50 = 2.56 µM; PKB: IC50 = 45 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
24882589
SMILES :
CC1=NC2=CN=C3C=CC(=CC3=C2N1C4=CC=C(C=C4)C(C)(C)C#N)C#CC5=CN=CC=C5

Download SDS (MSDS)

Certificate of Analysis

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