Tirabrutinib hydrochloride
Based on 8 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 1439901-97-9
- Formula: C25H23ClN6O3
- Molecular Weight:490.94
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tirabrutinib hydrochloride
More- Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- iScience. 2024 Sep 24;27(11):110961. [Abstract]
- ACS Pharmacol Transl Sci. 2025 Mar 12;8(4):917-931. [Abstract]
- Rapid Commun Mass Spectrom. 2022 Mar 15;36(5):e9240. [Abstract]
- bioRxiv. 2026 May 8:2026.05.07.723540. [Abstract]
- bioRxiv. 2024 September 08.
- bioRxiv. 2024 Oct 10:2023.12.18.572223. [Abstract]
- bioRxiv. 2023 Feb 24.
Biological Activity
|
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) |
Tirabrutinib hydrochloride (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 hydrochloride (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 hydrochloride (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.
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Cell Line:SU-DHL-6 and OCI-L Y10 cells
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Concentration:0.1-1000 nM; 0.001 nM-100 nM.
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Incubation Time:72 h
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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.
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Cell Line:SU-DHL-6 cells
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Concentration:0.5, 5, 50 μM
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Incubation Time:24, 48 h
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Result:Induced cell apoptosis when concentration up to 50 μM and incubated for 48 h.
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Cell Line:TMD8 cells
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Concentration:300 nM
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Incubation Time:72 h
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Result:Induced caspase-3 and PARP cleavage.
Tirabrutinib hydrochloride (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.
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Animal Model:Male SD rats (219.0–260.5g)[1].
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Dosage:10 mg/kg
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Administration:Oral administration; single.
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Result:
1.19 Pharmacokinetic Parameters of Tirabrutinib in male SD rats[1].
Plasma, Cmax (ng/mL) Brain, Cmax (ng/mL) Penetration rate
(%, Cmax,brain/Cmax,plasma)PO (10 mg/kg) 339.53 28.9 8.5
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Animal Model:Immunodeficiency (SCID) mice (mouse xenograft model)[2].
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Dosage:6, 20 mg/kg
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Administration:Oral administration; single daily for 3 weeks.
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Result:Inhibited tumour growth, and when dosage up to 20 mg/kg, a complete tumor suppression at day 14.
Chemical Information
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CAS No. 1439901-97-9
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Appearance Solid
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Molecular Weight 490.94
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Formula C25H23ClN6O3
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Color White to off-white
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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
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Synonyms
ONO-4059 hydrochloride; GS-4059 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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Stem Cell Reports
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 -
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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 -
Solvent & Solubility
DMSO : 100 mg/mL (203.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.79 mg/mL (3.65 mM); Clear solution
This protocol yields a clear solution of ≥ 1.79 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.9 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0369 mL | 10.1845 mL | 20.3691 mL | 50.9227 mL |
| 5 mM | 0.4074 mL | 2.0369 mL | 4.0738 mL | 10.1845 mL | |
| 10 mM | 0.2037 mL | 1.0185 mL | 2.0369 mL | 5.0923 mL | |
| 15 mM | 0.1358 mL | 0.6790 mL | 1.3579 mL | 3.3948 mL | |
| 20 mM | 0.1018 mL | 0.5092 mL | 1.0185 mL | 2.5461 mL | |
| 25 mM | 0.0815 mL | 0.4074 mL | 0.8148 mL | 2.0369 mL | |
| 30 mM | 0.0679 mL | 0.3395 mL | 0.6790 mL | 1.6974 mL | |
| 40 mM | 0.0509 mL | 0.2546 mL | 0.5092 mL | 1.2731 mL | |
| 50 mM | 0.0407 mL | 0.2037 mL | 0.4074 mL | 1.0185 mL | |
| 60 mM | 0.0339 mL | 0.1697 mL | 0.3395 mL | 0.8487 mL | |
| 80 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.6365 mL | |
| 100 mM | 0.0204 mL | 0.1018 mL | 0.2037 mL | 0.5092 mL |
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