ONO-4059 is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 2.2 nM).1 It is selective for BTK over LCK, LYN, and Fyn at 1 ?M.2 ONO-4059 inhibits B cell proliferation and activation in vitro and reduces tumor growth in a TMD8 mouse xenograft model.1,3
1.Burger, A.Bruton's tyrosine kinase (BTK) inhibitors in clinical trialsCurr. Hematol. Malig. Rep.9(1)44-49(2014) 2.Yasuhiro, T., Yoshizawa, T., Daub, H., et al.Abstract 2021: ONO-WG-307, a novel, potent and selective inhibitor of Bruton's tyrosine kinase (Btk), results in sustained inhibition of the ERK, AKT and PKD signaling pathwaysCancer Res.72(8 Supplement)2021(2012) 3.Kozaki, R., Yoshizawa, T., Tohda, S., et al.Abstract 3731: Development of a Bruton's tyrosine kinase (Btk) inhibitor, ONO-WG-307: Efficacy in ABC-DLBCL xenograft model – potential treatment for B-cell malignanciesBlood118(21)3731(2011)