Description: Tirabrutinib HCl (formerly known as ONO-4059; GS4059; ONO-WG-307; Steboronine), the hydrochloride salt of tirabrutinib, is a selective, covalent/irreversible and orally bioavailable BTK inhibitor approved in Japan for cancer treatment. It inhibits BTK with an IC50 of 2.2 nM. Tirabrutinib covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
References: Blood, 2016 Jan 28, 127(4): 411-419.; Curr Hematol Malig Rep, 2014 Mar, 9(1):44-9.
Related CAS: 1351636-18-4 (free base); 1439901-97-9 (HCl); 1351635-67-0 (ONO-4059-analog)