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AZD2858 - CAS 486424-20-8

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AZD2858 is a potent and selective GSK3β inhibitor with Ki value of 4.9 nM. It was shown to promote osteoblast differentiation in human adipose-derived stem cells (hADSC) in vitro.

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Molecular Formula

C21H23N7O3S

Molecular Weight

453.52

AZD2858

- Specification
  - Purity
    
    >98%
    
    IUPAC Name
    
    3-amino-6-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]-N-pyridin-3-ylpyrazine-2-carboxamide
    
    Synonyms
    
    AZD-2858; 3-amino-6-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]-N-pyridin-3-ylpyrazine-2-carboxamide
- Properties
  - InChI Key
    
    FHCSBLWRGCOVPT-UHFFFAOYSA-N
    
    InChI
    
    InChI=1S/C21H23N7O3S/c1-27-9-11-28(12-10-27)32(30,31)17-6-4-15(5-7-17)18-14-24-20(22)19(26-18)21(29)25-16-3-2-8-23-13-16/h2-8,13-14H,9-12H2,1H3,(H2,22,24)(H,25,29)
    
    Canonical SMILES
    
    CN1CCN(CC1)S(=O)(=O)C2=CC=C(C=C2)C3=CN=C(C(=N3)C(=O)NC4=CN=CC=C4)N
- Reference Reading
  - 1.Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation.
    
    Sisask G1, Marsell R, Sundgren-Andersson A, Larsson S, Nilsson O, Ljunggren O, Jonsson KB. Bone. 2013 May;54(1):126-32. doi: 10.1016/j.bone.2013.01.019. Epub 2013 Jan 19.
    
    Fracture healing is a complex interplay between endochondral and intramembranous bone formation processes. The canonical Wnt/β-catenin pathway enhances new bone formation and may play a role in fracture healing. Glycogen synthase kinase 3β (GSK3β) is a key regulator of β-catenin degradation. In this study, we investigate the effects of AZD2858, an orally bioactive GSK3 inhibitor, on fracture healing. Femoral fractures were produced in rats after the insertion of a femoral nail. The rats were treated with oral administration of AZD2858 at a dose of 30 μmol/kg (20mg/kg) daily for up to 3 weeks, while control animals were administered vehicle. At 4days, and at 1, 2 and 3 weeks, histological analysis was performed, and at the 2 and 3 week time points, we performed peripheral quantitative computed tomography (pQCT), X-rays, and four-point bending tests. Peripheral QCT showed an increase in both mineral density (of 28% at 2 weeks and 38% at 3weeks) and mineral content (of 81% at 2 weeks and 93% at 3 weeks) in the calluses from AZD2858 treated animals as compared to vehicle treated animals.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 2.2050 mL 11.0249 mL 22.0497 mL
    
    5 mM 0.4410 mL 2.2050 mL 4.4099 mL
    
    10 mM 0.2205 mL 1.1025 mL 2.2050 mL
    
    50 mM - - -

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	2.2050 mL	11.0249 mL	22.0497 mL
5 mM	0.4410 mL	2.2050 mL	4.4099 mL
10 mM	0.2205 mL	1.1025 mL	2.2050 mL
50 mM	-	-	-

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