Ritlecitinib

MCE 国际站：Ritlecitinib

产品活性：Ritlecitinib (PF-06651600) 是一种口服有效的，选择性的 JAK3 抑制剂，IC₅₀ 值为 33.1 nM。

研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt

作用靶点：JAK

In Vitro: Ritlecitinib is a potent JAK3-selective inhibitor which can inhibit the JAK3 kinase activity with an IC₅₀ of 33.1 nM but without activity (IC₅₀>10 000 nM) against JAK1, JAK2, and TYK2. Ritlecitinib inhibits the phosphorylation of STAT5 elicited by IL-2, IL-4, IL-7, and IL-15 with IC₅₀ values of 244, 340, 407, and 266 nM, respectively. Ritlecitinib also inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC₅₀ of 355 nM. Functional assessment in T-cell differentiation assays demonstrate that Ritlecitinib suppresses Th1 and Th17 differentiation as measured by IFNγ, after 5 days under Th1 conditions, and IL-17 production, after 6 days under Th17 conditions, with IC₅₀ values of 30 nM and 167 nM, respectively. Ritlecitinib also suppresses Th1 and Th17 function as measured by the inhibition of IFNγ production (IC₅₀=48 nM) and IL-17 production (IC₅₀=269 nM) in cells that have been previously differentiated and rested before being treated with PF-06651600.

In Vivo: In the rat adjuvant-induced arthritis (AIA) model, Ritlecitinib reduces paw swelling with an unbound EC₅₀ of 169 nM. Similarly, Ritlecitinib significantly reduces disease severity in the experimental autoimmune encephalomyelitis (EAE) mouse model when dosed either therapeutically at 30 or 100 mg/kg or prophylactically at 20 and 60 mg/kg. The efficacy of Ritlecitinib in these two rodent models of inflammatory and autoimmune diseases illustrates that JAK3-selective inhibition can be sufficient to have disease modifying effects in human diseases.

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