Tirabrutinib (hydrochloride)

Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB) ), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies[1][2][3][4].

Product Specifications

CAS Number

[1439901-97-9]

Product Name Alternative

ONO-4059 (hydrochloride) ; GS-4059 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Apoptosis; Btk

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ONO-4059-hydrochloride.html

Purity

99.66

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C2=CC=C(OC3=CC=CC=C3)C=C2)C4=C(N)N=CN=C4N1[C@H]5CN(C(C#CC)=O)CC5.[H]Cl

Molecular Formula

C25H23ClN6O3

Molecular Weight

490.94

Precautions

H302, H315, H319

References & Citations

[1]Yu H, et al. Bruton's tyrosine kinase inhibitors in primary central nervous system lymphoma-evaluation of anti-tumor efficacy and brain distribution. Transl Cancer Res. 2021 May;10 (5) :1975-1983. |[2]Kozaki R, et al. Responses to the Selective Bruton's Tyrosine Kinase (BTK) Inhibitor Tirabrutinib (ONO/GS-4059) in Diffuse Large B-cell Lymphoma Cell Lines. Cancers (Basel) . 2018 Apr 23;10 (4) :127. |[3]Liclican A, et al. Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition. Biochim Biophys Acta Gen Subj. 2020 Apr;1864 (4) :129531. |[4]Dhillon S. Tirabrutinib: First Approval. Drugs. 2020 Jun;80 (8) :835-840.