BAG 956

Name: BAG 956
Brand: Tocris Bioscience
SKU: 3606

Tocris Bioscience, part of Bio-Techne | Catalog # 3606

COA / SDS

Dual PI 3-kinase and PDPK1 (PDK1) inhibitor

Key Product Details

Description:	Dual PI 3-kinase and PDPK1 (PDK1) inhibitor
Chemical Name:	α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
Purity:	≥98% (HPLC)
Molecular Weight:	427.5

View Full Technical Details for BAG 956

Technical Data
Citations

Biological Activity for BAG 956

BAG 956 is a 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.

Compound Libraries for BAG 956

BAG 956 is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for BAG 956

M. Wt	427.5
Formula	C₂₈H₂₁N₅
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	853910-02-8
PubChem ID	24882589
InChi Key	GVPAGJWVBUZHNQ-UHFFFAOYSA-N
Smiles	CC3=NC1=C(N3C4=CC=C(C(C)(C#N)C)C=C4)C2=C(C=CC(C#CC5=CN=CC=C5)=C2)N=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for BAG 956

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	17.1	40
	ethanol	8.55	20

Preparing Stock Solutions for BAG 956

The following data is based on the product molecular weight 427.5.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.4 mM	5.85 mL	29.24 mL	58.48 mL
2 mM	1.17 mL	5.85 mL	11.70 mL
4 mM	0.58 mL	2.92 mL	5.85 mL
20 mM	0.12 mL	0.58 mL	1.17 mL

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References for BAG 956

References are publications that support the biological activity of the product.

Weisberg Potentiation of antileukemic therapies by the dual PI3K/PDK-1 inhibitor, BAG956: effects on BCR-ABL- and mutant FLT3-expressing cells. Blood 2008 PMID: 18184863
Marone Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol.Cancer Res. 2009 PMID: 19372588
Stauffer Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg.Med.Chem.Lett. 2008 PMID: 18248814