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Submit ReviewBAG 956
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)
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 Data 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 | 11.7 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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Product Datasheets for BAG 956
References for BAG 956
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
If you know of a relevant reference for BAG 956, please let us know.
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Keywords: BAG 956, BAG 956 supplier, Dual, inhibitors, PDK, PDK1, PI3K, p110, inhibits, PI, 3-kinases, Signaling, Signalling, Phosphoinositide, Kinases, PIP2, Inositol, Lipids, cAMP, 3-phosphoinositide, dependent, protein, kinase-1, BAG956, PDPK1, 3-Kinase, Phosphoinositide-dependent, Kinase, 1, 3606, Tocris Bioscience
Citations for BAG 956
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