Cayman Ibrutinib

Bruton’s tyrosine kinase (BTK) is a member of the BTK/Tec family of protein tyrosine kinases involved in signal transduction pathways regulating proliferation, survival, migration, and tissue homing of B-cells.¹ Ibrutinib is an irreversible inhibitor of BTK (IC₅₀ = 0.5 nM) that selectively blocks B cell activation, promoting apoptosis and preventing homing to the protective tumor microenvironment, at concentrations that do not affect T cell receptor signaling (1,000-fold more potent).^2,3 It has been reported to inhibit autophosphorylation of BTK (IC₅₀ = 11 nM), phosphorylation of PLCγ (IC₅₀ = 29 nM), a substrate of BTK, and phosphorylation of ERK (IC₅₀ = 13 nM), a further downstream kinase.² Its use has been examined clinically for the treatment of diseases associated with B cell antigen receptor signaling, including mantle cell lymphoma, chronic lymphocytic leukemia, and non-Hodgkin lymphoma.^1,2,4

WARNING This product is not for human or veterinary use.