BAG 956

Key Product Details

Product Description

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.

Product Specifications for BAG 956

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

Solubility

Preparing Stock Solutions for BAG 956

The following data is based on the product molecular weight 427.50.

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

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

Product Documents for BAG 956