tirabrutinib(ONO-4059) hydrochloride

For research use only.

Catalog No.S8166 Synonyms: GS-4059

4 publications

tirabrutinib(ONO-4059) hydrochloride Chemical Structure

CAS No. 1439901-97-9

Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.

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Biological Activity

Description Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
BTK [1]
2.2 nM
In vitro

ONO-4059 covalently binds to BTK, and reversibly blocks BCR signaling and B-cell proliferation and activation[1]. 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[4].

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[1]. 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[3].


Cell Research:[2]
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  • Cell lines: DLBCL cell lines TMD8 cells
  • Concentrations: 320 nM
  • Incubation Time: 48 h
  • Method: Cells are treated with idelalisib (420 nM), ONO/GS-4059 (320 nM) or in combination for 48 hours and apoptosis is assessed by FITC Annexin V staining, and measured by flow cytometry
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Male CB17-SCID mice
  • Dosages: 5 and 10 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 98 mg/mL (199.61 mM)
Water Insoluble
Ethanol '1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 490.94


CAS No. 1439901-97-9
Storage powder
in solvent
Synonyms GS-4059
Smiles CC#CC(=O)N1CCC(C1)N2C3=NC=NC(=C3N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5)N.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02626026 Completed Drug: GS-4059|Drug: Placebo Rheumatoid Arthritis Gilead Sciences January 2016 Phase 1
NCT01659255 Completed Drug: ONO/GS-4059 Non Hodgkins Lymphoma|Chronic Lymphocytic Leukaemia Gilead Sciences|Ono Pharmaceutical Co. Ltd August 2012 Phase 1

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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID