BAG 956

Pricing Availability Delivery Time Qty
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
Literature

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.

Compound Libraries

BAG 956 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

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.

All Tocris products are intended for laboratory research use only.

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 solvent 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
1 mM 2.34 mL 11.7 mL 23.39 mL
5 mM 0.47 mL 2.34 mL 4.68 mL
10 mM 0.23 mL 1.17 mL 2.34 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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.

View Related Products by Product Action

View all PI 3-kinase Inhibitors

Keywords: 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 PI 3-Kinase

Citations for BAG 956

Citations are publications that use Tocris products.

Currently there are no citations for BAG 956. Do you know of a great paper that uses BAG 956 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling

Pathways for BAG 956

Protocols

TODO: Add Protocols