BMS 509744

An Itk inhibitor (IC50 = 19 nM), selective for Itk over 18 other kinases (IC50s = >1,100 nM for all), inhibits IL-2 secretion from Jurkat T cells and isolated human PBMCs induced by antibodies targeting CD3 (IC50s = 0.25 and 0.39 µM, respectively), decreases serum levels of Il-2 and the lung infiltration of total immune cells and eosinophils in a mouse model of ovalbumin-induced lung inflammation at 25 mg/kg, reduces ear skin thickness and decreases the number of infiltrating immune cells in a mouse model of imiquimod-induced skin inflammation when topically applied at 3%. Formulation: A solid. InChI: InChI=1S/C32H41N5O4S2/c1-20-16-26(41-7)25(30(40)37-14-12-36(13-15-37)22(3)38)17-27(20)42-28-19-34-31(43-28)35-29(39)24-10-8-23(9-11-24)18-33-21(2)32(4,5)6/h8-11,16-17,19,21,33H,12-15,18H2,1-7H3,(H,34,35,39). InChIKey: ZHXNIYGJAOPMSO-UHFFFAOYSA-N. SMILES: O=C(C1=CC=C(CNC(C(C)(C)C)C)C=C1)NC2=NC=C(SC3=C(C)C=C(OC)C(C(N4CCN(C(C)=O)CC4)=O)=C3)S2