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

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

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

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
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 55 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Tirabrutinib:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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].

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 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].

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.
SMILES

O=C1N(C2=CC=C(OC3=CC=CC=C3)C=C2)C4=C(N)N=CN=C4N1[[email protected]]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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (220.03 mM)

*"≥" 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
10 mM 0.2200 mL 1.1002 mL 2.2003 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.65%

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tirabrutinib
Cat. No.:
HY-15771
Quantity:
MCE Japan Authorized Agent: