BAG 956
Tocris Bioscience, part of Bio-Techne | Catalog # 3606
Dual PI 3-kinase and PDPK1 (PDK1) inhibitor
Discontinued Product
3606 has been discontinued.
View all PI 3-Kinase Inhibitors products.
Key Product Details
Description
Dual PI 3-kinase and PDPK1 (PDK1) inhibitor
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
Molecular Weight
427.50
Formula
C28H21N5
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
α,α,-Dimethyl-4-[2-methyl-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-benzeneacetonitrile
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.
Solubility
| 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 427.50
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for BAG 956
For research use only
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