| Identification | Back Directory | [Name]
AZD-2858 | [CAS]
486424-20-8 | [Synonyms]
AZD2858
AZD-2858
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-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-pyrazinecarboxamide AZD2858 | [Molecular Formula]
C21H23N7O3S | [MDL Number]
MFCD26397072 | [MOL File]
486424-20-8.mol | [Molecular Weight]
453.517 |
| Chemical Properties | Back Directory | [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 |
| Questions And Answer | Back Directory | [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. |
| Hazard Information | Back Directory | [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. | [IC 50]
GSK-3α: 0.9 nM (IC50); GSK-3β: 5 nM (IC50); CDK5/p25: 356 nM (IC50); Haspin: 366 nM (IC50); CDK5/p35: 387 nM (IC50); DYRK2: 491 nM (IC50); CDK2/cyclin A: 810 nM (IC50); CDK1/cyclin B: 1246 nM (IC50); PIM3: 1269 nM (IC50); TLK2: 1381 nM (IC50); PKD2: 2462 nM (IC50); CDK2/cyclin E: 3310 nM (IC50); Aurora-A: 4966 nM (IC50) | [storage]
Store at -20° C |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
|