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Selleckchem/PF-06700841/S8804

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S8804

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DescriptionPF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.TargetsJAK1 [1](Cell-free assay)Tyk2 [1](Cell-free assay)JAK2 [1](Cell-free assay)17 nM23 nM77 nMIn vivoThe pharmacokinetics of PF-06700841 are studied in Sprague−Dawley rats following intravenous and oral administration (1 and 3 mg/kg respectively) of the tosylate salt, where the compound shows a plasma clearance of 31 mL/min/kg, a volume of distribution of 2.0 L/kg, and oral bioavailability of 83%. Following the 3 mg/kg oral dose, the Cmax is 774 ng/mL and the AUC∞ is 1340 ng·h/mL. The high oral bioavailability indicates high absorption from the gut, consistent with its in vitro passive permeability properties and high solubility[1].

Selleck Chemicals是世界领先的高性能的生命科学产品供应商之一，主要致力于提供MAPK和PI3K/Akt/mTOR等上百个信号通路的高特异性小分子抑制剂。Selleck 产品线补充非常及时，可以提供行业内最新的抑制剂类产品。同时Selleck也是专业的高通量筛选抑制剂分子库、API、天然产物和多肽供应商。