Basic information Description In vitro In vivo Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  PI3K / Akt / mTOR >  GSK-3 inhibitors >  AZD-2858

AZD-2858

Basic information Description In vitro In vivo Safety Supplier Related

AZD-2858 Basic information

Product Name:
AZD-2858
Synonyms:
  • AZD 2858
  • AZD2858
  • AZD-2858
  • 3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-pyrazinecarboxamide
  • 2-Pyrazinecarboxamide, 3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-
  • 3-Amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-N-3-pyridinyl-pyrazinecarboxamide AZD2858
  • 3-Amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide
  • 3-Amino-6-{4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl}-N-(3-pyridinyl)-2-pyrazinecarboxamide
CAS:
486424-20-8
MF:
C21H23N7O3S
MW:
453.52
Product Categories:
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
Mol File:
486424-20-8.mol
More
Less

AZD-2858 Chemical Properties

Density 
1.408±0.06 g/cm3(Predicted)
storage temp. 
Store at -20° C
solubility 
DMSO:8.0(Max Conc. mg/mL);17.64(Max Conc. mM)
form 
A crystalline solid
pka
7.17±0.70(Predicted)
color 
Green to khaki
More
Less

AZD-2858 Usage And Synthesis

Description

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.

In vitro

AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, inhibits tau phosphorylation at the S396 site, activates Wnt signaling pathway. AZD2858 treatment (1 μM, 12 h) on primary isolated human osteoblast-like cells results in a 3-fold increase of β-catenin levels. AZD2858 causes β-catenin stabilisation in human and rat mesenchymal stem cells, stimulates hADSC commitment towards osteoblasts and osteogenic mineralisation in vitro.

In vivo

In rats, oral AZD2858 treatment causes a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect at a dose of 20 mg/kg once daily (total BMC: 172% of control). A small but significant effect is also seen at cortical sites (total BMC: 111% of control). AZD285 treatment (30 μmol/kg) on rats daily for up to 3 weeks shows an increase in both mineral density (of 28% at 2 weeks and 38% at 3 weeks) and mineral content (of 81% at 2 weeks and 93% at 3 weeks) in the calluses. AZD285 treatment makes the fractures heals more rapidly, with a bony callus without an obvious endochondral component. AZD2858 produces time-dependent changes in serum bone turnover biomarkers and increases bone mass over 28 days exposure in rats. After 7 days, AZD2858 increases the bone formation biomarker P1NP, and reduces the resorption biomarker TRAcP-5b, indicating increased bone anabolism and reduced resorption in rats.

Uses

AZD 2858 is a highly selective glycogen synthase kinase-3β (GSK3β) inhibitor used in the treatment of neurological diseases such as Alzheimer’s (1).

Definition

ChEBI: AZD2858 is a member of the class of pyrazines that is pyrazine substituted by (pyridin-3-yl)aminocarbonyl, amino, and 4-(4-methylpiperazine-1-sulfonyl)phenyl groups at positions 2, 3 and 6, respectively. It is a potent inhibitor of GSK3alpha and GSK3beta (IC50 values of 0.9 and 4.9 nM, respectively) and increases bone mass (via Wnt activation) in rats. It has a role as an EC 2.7.11.26 (tau-protein kinase) inhibitor, an antineoplastic agent, a bone density conservation agent and a Wnt signalling activator. It is a member of pyrazines, a secondary carboxamide, a member of pyridines, a N-methylpiperazine, a sulfonamide and an aromatic amine.

storage

Store at -20°C

AZD-2858Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Products Intro
Product Name:AZD-2858
CAS:486424-20-8
Purity:98% Package:1g,10g,100g,1kg
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)
Products Intro
Product Name:AZD2858
CAS:486424-20-8
Purity:99% Package:5Mg, 10Mg, 20Mg, 50Mg
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Products Intro
Product Name:AZD-2858
CAS:486424-20-8
Purity:>98% Package:100MG Remarks:4870
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
Products Intro
Product Name:AZD2858
CAS:486424-20-8
Purity:>98% Package:1116RMB/10mg
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Email
market@aladdin-e.com
Products Intro
Product Name:AZD2858
CAS:486424-20-8
Purity:10mM in DMSO Package:1ml/RMB 720.90