PF-06700841 (C007B-248928)

InformationPF-06700841 (PF-841) is a potent inhibitor ofTyk2andJak1with 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 (Cell-free assay); Tyk2 (Cell-free assay); JAK2 (Cell-free assay) 17 nM; 23 nM; 77 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. Specification: 10mM in DMSO Molecular Formula: C18H21F2N7O Molecular Weight: 389.4 PubChem CID: 118878093 Isomeric SMILES: CN1C=C(C=N1)NC2=NC=CC(=N2)N3C[C@H]4CC[C@@H](C3)N4C(=O)[C@@H]5CC5(F)F