Abrocitinib 是可口服、选择性的JAK1抑制剂，可用于自身免疫症的研究，对 JAK1 和 JAK2 的IC50值分别为 29 和 803 nM。它可抑制 TYK2 的活性，IC50为1.253 μM， 也可抑制刺激后 STAT1、STAT3 和 STAT5 的磷酸化水平。

Abrocitinib (PF-04965842) is a potent, specific and orally-active JAK1 inhibitor (IC50s: 29/803 nM for JAK1/2).

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

In the rat adjuvant-induced arthritis model, Abrocitinib (5, 15, 50 mg/kg, p.o., daily for 7 days) significantly reduces paw swelling.

1622902-68-4

C14H21N5O2S

323.41

PF-04965842

DMSO:120 mg/mL (371.05 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years