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ChemicalBook--->CAS DataBase List--->1439901-97-9

1439901-97-9

1439901-97-9 Structure

1439901-97-9 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]


GHS07,GHS09
[Signal word ]

Warning
[Hazard statements ]

H302-H400-H410
[Precautionary statements ]

P264-P270-P273-P301+P312-P330-P391-P501
Hazard InformationBack 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]

TargetValue
BTK 2.2 nM
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