產(chǎn)品目錄

規(guī)格	5mg 25mg
CAS	944118-01-8
別名
化學(xué)名	4-(((1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl)amino)-7H-pyrrolo[2,3-b]pyridine-5-carbimidic acid
分子式	C18H22N4O2
分子量	326.39
溶解度	DMF: 2 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 1 mg/ml
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Peficitinib (ASP015K) is an oral Janus kinase (JAK) inhibitor. It inhibits enzyme activities of JAK1, JAK2, JAK3 and Tyk2 with IC50 values of 3.9, 5.0, 0.71 and 4.8 nmol/L, respectively. It showed moderate selectivity for JAK3 inhibition [1].

JAK family of non-receptor protein tyrosine kinases includes JAK1, JAK2, JAK3 and tyrosine kinase 2 (Tyk2). JAK1, JAK2, JAK3 and Tyk2 are critically important in haematopoietic cells and immune cells [1].

Erythropoietin regulates haematopoiesis (the production of blood cells) [2]. Treatment with ASP015K inhibited the human T-cell proliferation induced by IL-2. And this effect was greater than the effect to inhibit EPO-induced human erythroleukemia cell proliferation. In human whole blood, ASP015K concentration-dependently inhibited STAT5 phosphorylation (pSTAT5) [3].

In healthy volunteers, STAT5-P was dose-dependently inhibited by ASP015K. When the doses of ASP015K were 60, 120, 200, or 300 mg, the mean peak percentage inhibitions of STAT5-P were 84%, 85%, 92%, and 93%, respectively. Plasma ASP015K inhibited STAT5-P with an EC50 value of 48 ng/mL, a shape factor (γ) of ~1.2, and an estimated Emax close to 100%. On days 1, 7, and 14, at ~2 hours after treatment with ASP015K at multiple doses, the peak of median percentage of STAT5-P inhibition appeared [4].

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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