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Abrocitinib(PF-04965842)
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Abrocitinib(PF-04965842)图片
CAS NO: 1622902-68-4
包装与价格:
包装 价格(元)
10mM (in 1mL DMSO) 电议
5mg 电议
10mg 电议

半岛bd体育手机客户端 介绍
Abrocitinib (PF-04965842) (PF-04965842) 是一种有效的、具有口服活性的选择性 JAK1 抑制剂,对 JAK1 和 JAK2 的 IC50 分别为 29 和 803 nM。
Cas No. 1622902-68-4
别名 PF-04965842(阿布罗替尼),PF-04965842
Canonical SMILES CN([C@H]1C[C@@H](NS(CCC)(=O)=O)C1)C2=C3C(NC=C3)=NC=N2
分子式 C14H21N5O2S
分子量 323.41
溶解度 DMSO : 125 mg/mL (386.51 mM)
储存条件 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
半岛bd体育手机客户端 描述

Abrocitinib (PF-04965842) is a potent, oral active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1,STAT3 and STAT5 after stimulation. Effective in autoimmune disease[1].

Abrocitinib (Compound 25) inhibits IFNα-stimulated phosphorylation of STAT3, IFN-stimulated phosphorylation of STAT1 in human whole blood (HWB), as well as pSTAT5 in CD34+ spiked into HWB (JAK2), with IC50s of 189, 163 nM, 7.178 μM, respectively[1].

[1]. Vazquez ML, et al. Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. J Med Chem. 2018 Feb 8;61(3):1130-1152.

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