[CAS NO. 1439901-97-9] tirabrutinib(ONO-4059) hydrochloride
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PRODUCTS SPECIFICATIONS [1439901-97-9]
Store
Catalog
SLK-S8166
Brand
Selleck
CAS
1439901-97-9
DESCRIPTION [1439901-97-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 490.94 |
| Molecular Formula | C25H22N6O3.HCl |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0369 mL | 10.1845 mL | 20.3691 mL |
| 5 mM | 0.4074 mL | 2.0369 mL | 4.0738 mL |
| 10 mM | 0.2037 mL | 1.0185 mL | 2.0369 mL |
| 50 mM | 0.0407 mL | 0.2037 mL | 0.4074 mL |
Description
Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective inhibitor with an IC50 of 2.2 nM.
Targets
| BTK [1] |
| 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.
References
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