- AZD2858
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- $32.00 / 1mg
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2025-07-03
- CAS:486424-20-8
- Min. Order:
- Purity: 98%
- Supply Ability: 10g
- AZD-2858
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- $2.00 / 1kg
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2019-07-06
- CAS:486424-20-8
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100kg
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| 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 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 |
| | 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. | | in vivo | AZD2858 (20 mg/kg) causes a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect[1]. AZD2858 exhibits a substantial effect on fracture healing. AZD2858 (20 mg/kg) causes an increase in cortical BMC of 9%, cortical area of 10%, and cortical thickness of 11% at 3 weeks in the non-operated right femur of rats[2]. AZD2858 (30 μmol/kg/day) alters the biomarkers of bone turnover with statistically significant increases in P1NP and decreases in TRAcP-5b seen from 3 days of treatment and onwards. AZD2858 demonstrates significant changes in serum bone turnover markers (P1NP and TRAcP-5b) and femur bone formation after only 7 days of daily dosing[3]. AZD2858 (AR28, 30 mg/kg, s.c.) stimulates an increase in an initial wave of mesenchymal progenitors with osteogenic and adipogenic potential and drives their differentiation to the osteogenic lineage in BALB/c mice. AR28 (30 mg/kg, s.c.) enhances the proliferation of committed hematopoietic progenitors and their differentiation to the osteoclast lineage but does not prevent an overall increase in bone mass[4]. | | 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 |
| | AZD-2858 Preparation Products And Raw materials |
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