AZD-2858

AZD-2858 Basic information
Description In vitro In vivo
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
EINECS:
Product Categories:Inhibitors;Akt;mTOR;PI3K
Mol File:486424-20-8.mol
AZD-2858 Structure
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
pka7.17±0.70(Predicted)
Safety Information
MSDS Information
AZD-2858 Usage And Synthesis
DescriptionAZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.
In vitroAZD2858 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 vivoIn 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.
UsesAZD 2858 is a highly selective glycogen synthase kinase-3β (GSK3β) inhibitor used in the treatment of neurological diseases such as Alzheimer’s (1).
DefinitionChEBI: 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.
storageStore at -20°C
AZD-2858 Preparation Products And Raw materials
Hesperadin IM-12 AZD-0156 (S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine KGZHRAVDXGQUQM-WCQGTBRESA-N AZD3839 hemifuMarate 2-Pyridinecarboxamide, 6-fluoro-5-[4-[(5-fluoro-3,4-dihydro-2-methyl-3-oxo-6-quinoxalinyl)methyl]-1-piperazinyl]-N-methyl- ABT 737 AZD 3759 AZD-5305 1-AZAKENPAULLONE TAK-285 AZD 1080 AZD-0284 AZD-8055 AZD5153 AZD-7648 CCR1 antagonist

Email:[email protected] [email protected]
Copyright © 2024 Mywellwork.com All rights reserved.