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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 |
|---|
| BIIB129
BIIB129 is a covalent, selective inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. |
| UBX-382
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. |
| GDC-0834
GDC-0834 is a potent and selective BTK inhibitor. |
| DD-03-171
DD-03-171 is a BTK, IKFZ1 and IKFZ3 degrader, the BTK IC50 a value of 5.1 nM. |
| N-piperidine Ibrutinib hydrochloride
N-piperidine Ibrutinib hydrochloride is a reversible Ibrutinib derivative. |
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