PF-06651600,1792180-81-4

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抑制剂描述：

产品名称：PF-06651600

产品别名：见爱必信官网

英文别名：PF-06651600

靶点：JAK

CAS：1792180-81-4

纯度：98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：PF-06651600 is a potent JAK3-selective inhibitor with an IC₅₀ of 33.1 nM.

溶解性：DMSO : 125 mg/mL (438.07 mM; Need ultrasonic)
H2O : 6.67 mg/mL (23.38 mM; Need ultrasonic)

体外研究：

PF-06651600 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. PF-06651600 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. PF-06651600 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 PF-06651600 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. PF-06651600 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.

体内研究：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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