CAS NO: | 1792180-81-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Ritlecitinib (PF-06651600) is an orally active and selectiveJAK3inhibitor with anIC50of 33.1 nM[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Ritlecitinib is a potent JAK3-selective inhibitor which can inhibit the JAK3 kinase activity with an IC50of 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 IC50values of 244, 340, 407, and 266 nM, respectively. Ritlecitinib also inhibits the phosphorylation of STAT3 elicited by IL-21 with an IC50of 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 IC50values 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[1]. | ||||||||||||||||
体内研究 (In Vivo) | In the rat adjuvant-induced arthritis (AIA) model, Ritlecitinib reduces paw swelling with an unbound EC50of 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[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 285.34 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C15H19N5O | ||||||||||||||||
CAS 号 | 1792180-81-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | 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
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以下溶剂前显示的百
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