BMS-509744 is an inhibitor of ATP competitive Itk (IC50: 19 nM).

ITK:19 nM

BMS-488516 and BMS-509744 effectively inhibit Itk in vitro, demonstrating IC50 values of 96 and 19 nM, respectively. Their competitive kinetics regarding ATP indicate binding to the ATP-binding site of the Itk kinase domain[1]. BMS-509744 also diminishes T-cell receptor-mediated responses, including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in human and mouse cells in vitro.

BMS-509744 demonstrates a 50% inhibitory effect at a dosage of 50 mg/kg, regardless of the induction antibody level. Both BMS-509744 and BMS-488516 inhibit IL-2 production triggered by anti-T-cell receptor antibody in mice. Moreover, BMS-509744 significantly reduces lung inflammation in a mouse model of ovalbumin-induced allergy/asthma[1].