ONO-4059 is a selective inhibitor ofBTK with IC50 2.2 nm, ONO-4059 binds toBTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
Tirabrutinib hydrochloride, known as ONO-4059 hydrochloride, is an orally bioavailable inhibitor of Bruton’s Tyrosine Kinase (BTK) capable of crossing the blood-brain barrier (BBB), with an IC50 of 6.8 nM. It forms an irreversible and covalent bond with BTK, inhibiting abnormal B cell receptor signaling pathways. This property makes tirabrutinib hydrochloride applicable for research into autoimmune diseases and hematological cancers[1].[2].[3].[4].
体内研究
In vivo, tirabrutinib hydrochloride demonstrates tumor growth inhibition with daily oral doses of 6 and 20 mg/kg over three weeks[2].
体外研究
In cell proliferation assays, tirabrutinib hydrochloride effectively inhibits the growth of OCI-LY10 and SU-DHL-6 cells with IC50 values of 9.127 nM and 17.10 nM, respectively, across a concentration range of 0.1-1000 nM or 0.001-100 nM over 72 hours[1].
High doses (up to 50 μM) and extended treatment times (48 hours) are required for tirabrutinib hydrochloride to induce apoptosis in SU-DHL-6 cells[1].
At 300 nM for 72 hours, it also triggers caspase-3 and PARP cleavage in TMD8 cells[2].
搜索
