ONO-4059 is a selective and novel inhibitor of BTK with IC50 2.2 nm, ONO-4059 binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. BTK is potently inhibited by ONO/GS-4059 with a 50% inhibitory concentration of 2 nmol/L. ONO -4059 induces classical apoptosis at nanomolar concentrations in the activated B-cell diffuse large B-cell lymphoma (DLBCL) cell line, TMD-822 and in a TMD-8 xenograft model, treatment with ONO -4059 resulted in inhibition of tumor growth.
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