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

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

Cat. No.: HY-15771A Purity: 99.43%
COA Handling Instructions

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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.

Tirabrutinib hydrochloride Chemical Structure

Tirabrutinib hydrochloride Chemical Structure

CAS No. : 1439901-97-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 88 In-stock
25 mg USD 165 In-stock
50 mg USD 275 In-stock
100 mg USD 450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

Other Forms of Tirabrutinib hydrochloride:

Tirabrutinib hydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[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 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.

Tirabrutinib hydrochloride 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 hydrochloride (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 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.

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

490.94

Formula

C25H23ClN6O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0369 mL 10.1845 mL 20.3691 mL
5 mM 0.4074 mL 2.0369 mL 4.0738 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, 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.

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  • Dilution Calculator

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    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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.09 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

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.43%

COA (257 KB) HNMR (274 KB) LCMS (266 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, 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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Tirabrutinib hydrochloride 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:

Tirabrutinib1439901-97-9ONO-4059GS-4059ONO4059ONO 4059GS4059GS 4059BtkApoptosisBruton tyrosine kinaseautoimmune disordershaematological malignanciesPCNSLRAB cellsInhibitorinhibitorinhibit

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