Abrocitinib(PF-04965842)是一种有效、可口服、选择性的JAK1抑制剂，对JAK1和JAK2的IC50值分别为29和803nM。Abrocitinib(PF-04965842)可抑制TYK2的活性(IC50，1.253μM)和刺激后STAT1，STAT3和STAT5的磷酸化水平。可用于自身免疫症的研究。
CAS：1622902-68-4
分子式：C14H21N5O2S
分子量：323.41
纯度：98%
存储：Store at -20°C

Background:

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.