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In vitro: Tirabrutinib (ONO-4059) covalently bonds to BTK, inhibiting BCR signaling and B-cell proliferation and activation. Tirabrutinib (ONO-4059) induced durable responses in relapsed/refractory B-cell malignancies without significant toxicities.
In vivo: Tirabrutinib (ONO-4059) demonstrated therapeutic efficacy in a mouse arthritis model, and based on its anti-proliferative activity in B-cells.
| Molecular Weight | 454.48 |
| Formula | C25H22N6O3 |
| CAS Number | 1351636-18-4 |
| Solubility (25°C) | 10mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BTK Products |
|---|
| PCI-32765
PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| Spebrutinib (AVL-292)
Spebrutinib (AVL-292) is an oral, potent and selective small molecule covalent inhibitor of Btk (IC50 < 0.5 nM). |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
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