Abrocitinib (PF-04965842) (C09-0735-645)

InformationPF-04965842 is a potentJAK1inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.TargetsJAK1 (Cell-free assay); JAK2 (Cell-free assay); TYK2 (Cell-free assay) 29 nM; 803 nM; 1.253 μMIn vivoPhysicochemical properties and pharmacokinetic parameters of PF-04965842 are examined in rats following doses of 1 mg/kg iv or 3 mg/kg po. Clearance of PF-04965842 is low relative to total liver blood flow (CL = 26.6 mL/min/kg). Vdss = 1.04 L/kg. T1/2 = 1.1 h. The oral availability of PF-04965842 is 95.6%. PF-04965842 demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model. Specification: 0.97 Molecular Formula: C14H21N5O2S Molecular Weight: 323.41 EC Number: 817-215-8 PubChem CID: 78323835 Isomeric SMILES: CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3