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

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
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 61 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 99 In-stock
Estimated Time of Arrival: December 31
25 mg USD 165 In-stock
Estimated Time of Arrival: December 31
50 mg USD 275 In-stock
Estimated Time of Arrival: December 31
100 mg USD 495 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

Other Forms of Tirabrutinib hydrochloride:

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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].

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 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].

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

Appearance

Solid

Formula

C25H23ClN6O3
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.[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)

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
10 mM 0.2037 mL 1.0185 mL 2.0369 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

  • 3.

    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

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

Purity: 99.43%

COA (257 KB) HNMR (274 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
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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.

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Keywords:

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

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