2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Btk Apoptosis
  4. Tirabrutinib

Tirabrutinib  (Synonyms: ONO-4059; GS-4059)

Cat. No.: HY-15771 Purity: 99.65%
SDS COA Handling Instructions

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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.

Tirabrutinib Chemical Structure

Tirabrutinib Chemical Structure

CAS No. : 1351636-18-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 90 In-stock
25 mg USD 150 In-stock
50 mg USD 250 In-stock
100 mg USD 450 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Tirabrutinib:

Tirabrutinib Related Antibodies

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  • Purity & Documentation

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Description

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[1][2][3][4].

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.

Tirabrutinib Related Antibodies

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 Cmax (blood Cmax =339.53 ng/mL; brain Cmax =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, Cmax (ng/mL) Brain, Cmax (ng/mL) Penetration rate
(%, Cmax,brain/Cmax,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
Molecular Weight

454.48

Formula

C25H22N6O3
CAS No.
Appearance

Solid

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
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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2003 mL 11.0016 mL 22.0032 mL
5 mM 0.4401 mL 2.2003 mL 4.4006 mL
View the 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, 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.65%

SDS (393 KB)

COA (256 KB) HNMR (295 KB) LCMS (271 KB)

Handling Instructions (2659 KB)
References

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, 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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Tirabrutinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tirabrutinib1351636-18-4ONO-4059 GS-4059ONO4059ONO 4059GS4059GS 4059GS-4059BtkApoptosisBruton tyrosine kinaseautoimmune disordershaematological malignanciesPCNSLRAB cellsInhibitorinhibitorinhibit

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