Information tirabrutinib(ONO-4059) hydrochloride Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM. Targets BTK 2.2 nM In vitro ONO-4059 covalently binds to BTK, and reversibly blocks BCR signaling and B-cell proliferation and activation. It has greater selectivity for BTK than Lck, Fyn, LynA and ONO/GS-4059 only inhibits anti-IgM-induced B-cell activation in a concentration-dependent manner but not inhibit anti-CD3/CD28-induced activation of T-lymphocytes from human PBMCs. ONO/GS-4059 inhibits cell proliferation in some malignant B-cell lines but also induces classical apoptosis at nanomolar concentration in the activated-B cell (ABC) DLBCL cell line, TMD8. In vivo ONO-4059 demonstrates therapeutic efficacy in a mouse CIA model by suppressing generation of inflammatory chemokines and cytokines including IL-6, IL-8, and TNFα by monocytes, and accompanied by regression of cartilage erosion, bone damage, and pannus formation. In pre-clinical models, and in the clinic in both CLL and NHL patients, It exerts its anti-tumour activity, with a favourable safety profile along with promising efficacy over a long duration. Cell Research(from reference) Cell lines：DLBCL cell lines TMD8 cells Concentrations：320 nM Incubation Time：48 h
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tirabrutinib(ONO-4059) hydrochloride
CAS number：1439901-97-9 molecular formula：C25H22N6O3.HCl
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| Chinese alias | - | ||
| English alias | 1439901-97-9 | ONO-4059 (GS-4059) hydrochloride | Tirabrutinib HCl | GS-4059 (hydrochloride) | UNII-U374135N48 | 6-amino-9-[(3R)-1-but-2-ynoylpyrrolidin-3-yl]-7-(4-phenoxyphenyl)purin-8-one;hydrochloride | ONO-4059 HCl | Tirabrutinib hydrochloride (JAN) | | ||
| CAS number | 1439901-97-9 | molecular formula | C25H22N6O3.HCl |
| molecular weight | 490.94 g/mol | Exact mass | ≥98% |
| PSA | 105.000 Ų | logp | 3.706 |
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