AZD 2858

Name: AZD 2858
Brand: Tocris Bioscience
SKU: 7650

Tocris Bioscience, part of Bio-Techne | Catalog # 7650

COA / SDS

Highly potent GSK-3 inhibitor; inhibits tau phosphorylation

Key Product Details

Description:	Highly potent GSK-3 inhibitor; inhibits tau phosphorylation
Chemical Name:	3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-2-pyrazinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	453.52

View Full Technical Details for AZD 2858

Technical Data
Citations

Biological Activity for AZD 2858

AZD 2858 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor (IC₅₀ values are 0.9 and 5 nM for GSK-3α and GSK-3β, respectively). AZD 2858 inhibits tau phosphorylation in vitro (IC₅₀ = 76 nM), improves fracture healing and increases bone mass in rodent models of bone fracture. Also activates Wnt signaling in vitro and in vivo. Brain permeable and orally bioavailable.

Technical Data for AZD 2858

M. Wt	453.52
Formula	C₂₁H₂₃N₇O₃S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	486424-20-8
PubChem ID	10138980
InChi Key	FHCSBLWRGCOVPT-UHFFFAOYSA-N
Smiles	O=C(NC=1C=NC=CC1)C=2N=C(C=NC2N)C3=CC=C(C=C3)S(=O)(=O)N4CCN(C)CC4

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 for AZD 2858

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	4.54	10

Preparing Stock Solutions for AZD 2858

The following data is based on the product molecular weight 453.52.

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
0.1 mM	22.05 mL	110.25 mL	220.50 mL
0.5 mM	4.41 mL	22.05 mL	44.10 mL
1 mM	2.20 mL	11.02 mL	22.05 mL
5 mM	0.44 mL	2.20 mL	4.41 mL

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References for AZD 2858

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

Berg Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines. J.Med.Chem. 2012 PMID: 22489897
Cook Wnt-dependent osteogenic commitment of bone marrow stromal cells using a novel GSK3β inhibitor. Stem Cell Res. 2014 PMID: 24382458
Sisask Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone 2013 PMID: 23337038