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Tocris/BAG 956/3606/10/10 mg

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货号: 3606/10

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

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.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

Keywords: 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, PI, 3-Kinase, Inositol, Lipids, Phosphoinositide-dependent, Kinase, 1, PDK1, PI, 3-Kinase, Tocris Bioscience

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