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Tirabrutinib

Name: Tirabrutinib
Brand: TargetMol
SKU: TQ0236
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0236Cas No. 1351636-18-4

Alias Velexbru, ONO-4059, GS-4059

Tirabrutinib (GS-4059) (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.

Tirabrutinib

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Purity: 99.64%

Catalog No. TQ0236Alias Velexbru, ONO-4059, GS-4059Cas No. 1351636-18-4

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$43	In Stock	In Stock
25 mg	$73	In Stock	In Stock
50 mg	$119	In Stock	In Stock
100 mg	$223	-	In Stock
200 mg	$332	-	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.64%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Tirabrutinib (GS-4059) (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.
Targets&IC50	BLK:0.3 μM, ERBB2:7.31 μM, BTK:2.2 nM, JAK3:5.52 μM, ERB4:0.77 μM, TEC:48 nM, TXK:92 nM, BMX?kinase:6 nM, EGFR:3.02 μM
In vitro	Tirabrutinib (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-LY10 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 apoptosis in SU-DHL-6 cells, requiring high dosage and prolonged administration (up to 50 μM for 48 h)[1]. Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells[2].
In vivo	Tirabrutinib (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, reaching Cmax (blood Cmax = 339.53 ng/mL; brain Cmax = 28.9 ng/mL) 2 hours post-administration[1]. Additionally, Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) inhibits tumor growth in vivo[2].
Synonyms	Velexbru, ONO-4059, GS-4059

Chemical Properties

Molecular Weight	454.48
Formula	C₂₅H₂₂N₆O₃
Cas No.	1351636-18-4
Smiles	CC#CC(=O)N1CC[C@H](C1)n1c2ncnc(N)c2n(-c2ccc(Oc3ccccc3)cc2)c1=O
Relative Density.	1.412 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90 mg/mL (198.03 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.26 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2003 mL	11.0016 mL	22.0032 mL	110.0158 mL
5 mM	0.4401 mL	2.2003 mL	4.4006 mL	22.0032 mL
10 mM	0.2200 mL	1.1002 mL	2.2003 mL	11.0016 mL
20 mM	0.1100 mL	0.5501 mL	1.1002 mL	5.5008 mL
50 mM	0.0440 mL	0.2200 mL	0.4401 mL	2.2003 mL
100 mM	0.0220 mL	0.1100 mL	0.2200 mL	1.1002 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc