BI1002494 trifluoroacetate

A novel, potent, and selective spleen tyrosine kinase (SYK) inhibitor with enzyme IC50 of 30 nM, cell IC50 of 7 nM (FcεR1-mediated histamine release in human monocyte-derived mast cells, in the presence of 0.1% albumin); inhibits high-affinity IgE receptor-mediated mast cell and basophil degranulation (IC50=115 nM), 7-fold lower potency for blocking CD69 expression after anti-IgD (BCR) stimulation of peripheral B cells; dose-dependently inhibited OVA-induced bronchioalveolar lavage eosinophils in brown Norway rats.

References 1. Lamb DJ, et al. J Pharmacol Exp Ther. 2016 Jun;357(3):554-61. View Related Products by Target Syk