Description
PCI-32765 Racemate is a potent and highly selective inhibitor of Bruton tyrosine kinase (BTK), modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. It is a covalent and irreversible inhibitor of BTK through bonding to Cys-481 in the ATP binding domain. It inhibits phosphorylation of BTK in a B cells as well as the downstream substrates phosphoinositide phospholipase Cγ (PLC γ) and ERK in cell assays. It has in vivo efficacy in B cell lymphoma and efficacious in autoimmune disease. It also diminished FcγRIII-induced production of pro-inflammatory cytokines