Cat. No.: HY-15771

Tirabrutinib

(Synonyms: ONO-4059; GS-4059)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Tirabrutinib (ONO-4059) 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 irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.

For research use only. We do not sell to patients.

Purity: 99.71%
CAS No.: 1351636-18-4
Formula: C₂₅H₂₂N₆O₃
Molecular Weight:454.48

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tirabrutinib Chemical Structure

CAS No.: 1351636-18-4

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

BMX

6 nM (IC₅₀)

BTK

6.8 nM (IC₅₀)

TEC

48 nM (IC₅₀)

TXK

92 nM (IC₅₀)

BLK

0.3 μM (IC₅₀)

ERBB4

0.77 μM (IC₅₀)

EGFR

3.02 μM (IC₅₀)

JAK3

5.52 μM (IC₅₀)

ERBB2

7.31 μM (IC₅₀)

In Vitro

Tirabrutinib (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-L Y10 and SU-DHL-6 cells with IC₅₀s of 9.127 nM, and 17.10 nM, respectively^[1].
Tirabrutinib (0.5, 5, 50 μM; 24, 48 h) induces SU-DHL-6 cells apoptosis needs high dosage and prolonged administration (concentration up to 50 μM and incubates for 48 h)^[1].
Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

SU-DHL-6 and OCI-L Y10 cells
Concentration:

0.1-1000 nM; 0.001 nM-100 nM
Incubation Time:

72 h
Result:

Showed good anti-proliferative activity with IC₅₀s of 9.127 nM, and 17.10 nM for OCI-L Y10 and SU-DHL-6 cells, respectively.

Apoptosis Analysis^[1]

Cell Line:

SU-DHL-6 cells
Concentration:

0.5, 5, 50 μM
Incubation Time:

24, 48 h
Result:

Induced cell apoptosis when concentration up to 50 μM and incubated for 48 h.

Western Blot Analysis^[2]

Cell Line:

TMD8 cells
Concentration:

300 nM
Incubation Time:

72 h
Result:

Induced caspase-3 and PARP cleavage.

In Vivo

Tirabrutinib (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, and reaches C_max (blood C_max =339.53 ng/mL; brain C_max =28.9 ng/mL) 2 hours post administration^[1].
Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) shows inhibition of tumour growth in vivo^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male SD rats (219.0–260.5g)^[1].
Dosage:

10 mg/kg
Administration:

Oral administration; single.
Result:

1.19 Pharmacokinetic Parameters of Tirabrutinib in male SD rats^[1].

Plasma, C_max (ng/mL) Brain, C_max (ng/mL) Penetration rate
(%, C_max,_brain/C_max,_plasma)

PO (10 mg/kg) 339.53 28.9 8.5

Animal Model:

Immunodeficiency (SCID) mice (mouse xenograft model)^[2].
Dosage:

6, 20 mg/kg
Administration:

Oral administration; single daily for 3 weeks.
Result:

Inhibited tumour growth, and when dosage up to 20 mg/kg, a complete tumor suppression at day 14.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1351636-18-4
Appearance Solid
Molecular Weight 454.48
Formula C₂₅H₂₂N₆O₃
Color White to yellow
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
Synonyms

ONO-4059; GS-4059
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

Stem Cell Reports

Ibrutinib Displays Atrial-Specific Toxicity in Human Stem Cell-Derived Cardiomyocytes. [Abstract]

2019 May 14;12(5):996-1006. PMID: 31031187
iScience

Inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746. [Abstract]

2024 Sep 24;27(11):110961. PMID: 39759071
ACS Pharmacol Transl Sci

Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]

2025 Mar 12;8(4):917-931. PMID: 40242575
Rapid Commun Mass Spectrom

Characterization of the metabolites of tirabrutinib generated from rat, dog and human liver microsomes using ultra-high-performance liquid chromatography combined with high-resolution mass spectrometry. [Abstract]

2022 Mar 15;36(5):e9240. PMID: 34904306
bioRxiv

More than an attachment module: covalent inhibitor warheads influence BTK dynamics and function. [Abstract]

2026 May 8:2026.05.07.723540. PMID: 42146433
bioRxiv

2024 September 08.
bioRxiv

Impact of the clinically approved BTK inhibitors on the conformation of full-length BTK and analysis of the development of BTK resistance mutations in chronic lymphocytic leukemia. [Abstract]

2024 Oct 10:2023.12.18.572223. PMID: 38187560
bioRxiv

2023 Feb 24.

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (220.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2003 mL

11.0016 mL

22.0032 mL

5 mM

0.4401 mL

2.2003 mL

4.4006 mL

10 mM

0.2200 mL

1.1002 mL

2.2003 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[4]. Dhillon S. Tirabrutinib: First Approval. Drugs. 2020 Jun;80(8):835-840. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2003 mL	11.0016 mL	22.0032 mL	55.0079 mL
	5 mM	0.4401 mL	2.2003 mL	4.4006 mL	11.0016 mL
	10 mM	0.2200 mL	1.1002 mL	2.2003 mL	5.5008 mL
	15 mM	0.1467 mL	0.7334 mL	1.4669 mL	3.6672 mL
	20 mM	0.1100 mL	0.5501 mL	1.1002 mL	2.7504 mL
	25 mM	0.0880 mL	0.4401 mL	0.8801 mL	2.2003 mL
	30 mM	0.0733 mL	0.3667 mL	0.7334 mL	1.8336 mL
	40 mM	0.0550 mL	0.2750 mL	0.5501 mL	1.3752 mL
	50 mM	0.0440 mL	0.2200 mL	0.4401 mL	1.1002 mL
	60 mM	0.0367 mL	0.1834 mL	0.3667 mL	0.9168 mL
	80 mM	0.0275 mL	0.1375 mL	0.2750 mL	0.6876 mL
	100 mM	0.0220 mL	0.1100 mL	0.2200 mL	0.5501 mL

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	Plasma, C_max (ng/mL)	Brain, C_max (ng/mL)	Penetration rate (%, C_max,_brain/C_max,_plasma)
PO (10 mg/kg)	339.53	28.9	8.5

Tirabrutinib

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Publications Citing Use of MedChemExpress (MCE) Tirabrutinib

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tirabrutinib Related Classifications

Cat. No.: HY-15771