BAG 956

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Cat.No. 3606 - BAG 956 | C28H21N5 | CAS No. 853910-02-8
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: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

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
Storage Store at RT
Purity ≥99% (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 Data

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

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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 11.7 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

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

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


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Citations for BAG 956

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Literature in this Area

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