Abrocitinib CAS# 1622902-68-4 (cis-isomer) PF-04965842(阿布罗替尼)

Abrocitinib, an oral selective Janus kinase 1 (JAK1) inhibitor, showed potent preclinical activity in modulating cytokine signaling relevant to inflammatory diseases. In enzymatic assays, it inhibited JAK1 with an IC₅₀ of 29 nM, demonstrating 28-fold selectivity over JAK2, 340-fold over JAK3, and >130-fold over TYK2. In human peripheral blood mononuclear cells, abrocitinib suppressed IL-4–, IL-13–, and IL-31–induced STAT phosphorylation with IC₅₀ values ranging from 35 to 95 nM. In murine models of dermatitis, oral dosing reduced scratching behavior and inflammatory cytokine levels in a dose-dependent manner. These findings established its efficacy and selectivity, justifying advancement to clinical trials.