Identification | Back Directory | [Name]
ONO-4059 (hydrochloride) | [CAS]
1439901-97-9 | [Synonyms]
ON 0459 ON-0459 ONO-WG-307 ONO-4059 HCl ON 0459;ON-0459 Tirabrutinib HCl ONO-4059(HCl salt) GS-4059 (hydrochloride) ONO-4059 (hydrochloride) Tirabrutinib hydrochloride Tirabrutinib (ONO-4059) HCl ONO-4059(GS4059) hydrochloride TIRABRUTINIB (ONO-4059) HYDROCHLORIDE tirabrutinib(GS-4059/ONO-4059) hydrochloride TIRABRUTINIB HYDROCHLORIDE;GS-4059 (HYDROCHLORIDE) (R)-6-amino-9-(1-but-2-ynoylpyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one (R)-6-amino-9-(1-but-2-ynoylpyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one HCl salt ONO-4059 HCL; ONO4059; ONO 4059; ONO-4059; GS 4059; GS-4059; GS4059; ONO-WG-307; TIRABRUTINIB (R)-6-amino-9-(1-(but-2-ynoyl)pyrrolidin-3-yl)-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride | [EINECS(EC#)]
946-274-3 | [Molecular Formula]
C25H23ClN6O3 | [MDL Number]
MFCD30187521 | [MOL File]
1439901-97-9.mol | [Molecular Weight]
490.95 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 1 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | [form ]
A crystalline solid | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
ONO-4059 hydrochloride is a potent orally active BTK (Bruton's tyrosine kinase) inhibitor, IC50: 2.2nM.It is a potent and orally active Bruton agammaglobulinemia tyrosine kinase (BTK) in hibitor. Upon administration,it covalently binds to BTK within B cells,thereby preventing B-cell receptor signaling and impeding B-cell development. | [Biological Activity]
Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with IC50 of 2.2 nM. | [in vitro]
Compared with Lck, Fyn, LynA, ONO-4059 is more selective for BTK, and only inhibits anti-IgM-induced B cell activation in a concentration-dependent manner, but not anti-CD3/CD28-induced Activation of human PBMCs to T lymphocytes. ONO/GS-4059 inhibited cell proliferation in some malignant B cells, but also in the nanomolar concentration range, induced the classical apoptotic response of TMD8 cells. | [in vivo]
In the CIA mouse model, ONO-4059 exerted its curative effect by inhibiting the production of inflammatory chemokines and cytokines such as IL-6, IL-8, TNFalpha, etc. in monocytes, accompanied by cartilage erosion, bone damage, vascular Recession of nebula formation. In preclinical animal models and clinical CLL and NHL patients, ONO-4059 has antitumor activity, good safety and long-lasting efficacy. | [target]
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Company Name: |
Twochem Co.Ltd
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Tel: |
021-021-58111628 15800915896 |
Website: |
www.twochem.com |
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