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。

Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC 50 of 33.1 nM.

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JAK3 33.1 nM (IC50)

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

In the rat adjuvant-induced arthritis (AIA) model, Ritlecitinib reduces paw swelling with an unbound EC 50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Telliez JB, et al. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451.

In Vitro: DMSO : 125 mg/mL (438.07 mM; Need ultrasonic)H₂O : 6.67 mg/mL (23.38 mM; Need ultrasonic)配制储备液