Home Angiogenesis BTK inhibitor tirabrutinib(ONO-4059) hydrochloride For research use only.

tirabrutinib(ONO-4059) hydrochloride

Synonyms: GS-4059

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

tirabrutinib(ONO-4059) hydrochloride Chemical Structure

tirabrutinib(ONO-4059) hydrochloride Chemical Structure

CAS: 1439901-97-9

Selleck's tirabrutinib(ONO-4059) hydrochloride has been cited by 9 publications

Purity & Quality Control

Batch: S816601 DMSO] 98 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.77%
99.77

tirabrutinib(ONO-4059) hydrochloride Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Choose Selective BTK Inhibitors

Biological Activity

Description Tirabrutinib Hydrochloride (ONO-4059, GS-4059) is a highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
Targets
BTK [1]
2.2 nM
In vitro
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].
Cell Research 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
In Vivo
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].
Animal Research Animal Models Male CB17-SCID mice
Dosages 5 and 10 mg/kg
Administration by oral gavage

Chemical Information & Solubility

Molecular Weight 490.94 Formula

C25H22N6O3.HCl
CAS No. 1439901-97-9 SDF Download tirabrutinib(ONO-4059) hydrochloride SDF
Smiles CC#CC(=O)N1CCC(C1)N2C3=NC=NC(=C3N(C2=O)C4=CC=C(C=C4)OC5=CC=CC=C5)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 98 mg/mL ( (199.61 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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