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AZD2858

目录号: PL04524 纯度: ≥99%

AZD2858 是一种有效的，可口服的 GSK-3 抑制剂，可以抑制 GSK-3α 和 GSK-3β 的活性，IC50 值分别为 0.9 和 5 nM，可用于骨折愈合的研究。

CAS No. :486424-20-8

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PL04524-10mg	10mg	¥832.00	请登录
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PL04524-100mg	100mg	¥3965.00	请登录
PL04524-200mg	200mg	询价	询价
PL04524-10mM*1mLinDMSO	10mM*1mLinDMSO	¥1973.00	请登录
PL04524-1 mL x 10 mM (in DMSO)		¥885.00	请登录

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中文名称	AZD2858
中文别名	3-氨基-6-(4-((4-甲基-1-哌嗪基)磺酰基)苯基)-N-3-吡啶基-吡嗪甲酰胺;3-氨基-6-[4-(4-甲基哌嗪-1-基)磺酰基苯基]-n-吡啶-3-基吡嗪-2-羧酰胺;3-氨基-6-[4-[(4-甲基-1-哌嗪基)磺酰基]苯基]-N-3-吡啶基-吡嗪甲酰胺;AZD2858 抑制剂
英文名称	AZD2858
英文别名	AZD2858;3-amino-6-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]-N-pyridin-3-ylpyrazine-2-carboxamide;3-Amino-6-{4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl}-N-(3-pyrid inyl)-2-pyrazinecarboxamide;AZD 2858;AZD-2858;AZD 2858;3-amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide;3-Amino-6-{4-[(4-Methylpiperazin-1-Yl)sulfonyl]phenyl}-N-Pyridin-3-Ylpyrazine-2-Carboxamide;GSK-3 inhibition;3-amino-6-{4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-N-(pyridin-3-yl)pyrazine-2-carboxamide;GTPL8478;C21H23N7O3S;AOB6850;FHCSBLWRG
Cas No.	486424-20-8
分子式	C₂₁H₂₃N₇O₃S
分子量	453.52
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	AZD2858 是一种有效的，可口服的 GSK-3 抑制剂，可以抑制 GSK-3α 和 GSK-3β 的活性，IC50 值分别为 0.9 和 5 nM，可用于骨折愈合的研究。

产品详情	AZD2858 是一种有效的，可口服的 GSK-3 抑制剂，可以抑制 GSK-3α 和 GSK-3β 的活性，IC₅₀ 值分别为 0.9 和 5 nM，可用于骨折愈合的研究。
生物活性	AZD2858 is a potent, orally active GSK-3 inhibitor, with IC 50 s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
性状	Solid
IC50 & Target[1][2]	GSK-3α 0.9 nM (IC50) GSK-3β 5 nM (IC5
体外研究(In Vitro)	AZD2858 (1 μM) increases β-catenin levels after a short period of time in human osteoblast cells. AZD2858 inhibits GSK-3β dependent phosphorylation with an IC50 of 68 nM. AZD2858 (10 nM) has no effect on β-catenin levels. AZD2858 increases TAZ expression and osterix expression both by 1.4-fold, with EC50 of 440 nM and 1.2 μM, respectively, in hADSC. AZD2858 also induces a marked increase in osteogenic mineralisation in hADSC. AZD2858 (AR28) demonstrates from 70- to greater than 6000-fold selectivity over a panel of other kinases and an IC50 of 5 nM. AR28 inhibits GSK-3 in murine cells and indicates activation of the canonical Wnt/β-catenin signaling cascade. AR28 (50, 10, and 1 nM) enhances the clonogenic ability of mesenchymal progenitors with osteogenic and adipogenic potential. AR28 (50 μM) also enhances the differentiation ability of mesenc
体内研究(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. 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. 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. 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 oste
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Marsell R, et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012 Mar;50(3):619-27. [2]. Sisask G, et al. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone. 2013 May;54(1):126-32. [3]. Gilmour PS, et al. Huma

溶解度数据	In Vitro: DMSO : 12.5 mg/mL (27.56 mM; Need ultrasonic)配制储备液

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[1]. Marsell R, et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012 Mar;50(3):619-27.
[2]. Sisask G, et al. Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation. Bone. 2013 May;54(1):126-32.
[3]. Gilmour PS, et al. Huma

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

AZD2858

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