PF-4800567
目录号: PL13969 纯度: ≥98%
CAS No. :1188296-52-7
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中文名称
PF-4800567
中文别名
3-[(3-氯苯氧基)甲基]-1-(四氢-2H-吡喃-4-基)-1H-吡唑并[3,4-d]嘧啶-4-胺
英文名称
PF-4800567
英文别名
3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine;PF 4800567;PF-4800567
Cas No.
1188296-52-7
分子式
C17H18N5O2Cl
分子量
359.81
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-4800567 是一种有效、选择性的酪蛋白激酶 1ϵ (CK1ϵ) 抑制剂,IC50 值为 32 nM,对其选择性是对 CK1δ (IC50,711 nM) 的 20 倍。
生物活性
PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC 50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC 50 , 711 nM).
性状
Solid
IC50 & Target[1][2]
CKIδ 711 nM (IC50)
体外研究(In Vitro)
PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 shows inhibitory activity against CK1? and CK1δ in whole cells, with IC50s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1?-mediated PER3 nuclear localization mediated by CK1? and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Walton KM, et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9.
溶解度数据
In Vitro: DMSO : 75 mg/mL (208.44 mM; Need ultrasonic)配制储备液
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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。

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