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Tirabrutinib

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

🥰Excellent

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

🥰Excellent

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]

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Batch Information

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Purity:99.64%

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COA LCMS HNMR

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	TEC:48 nM, TXK:92 nM, ERBB2:7.31 μM, BLK:0.3 μM, BMX?kinase:6 nM, JAK3:5.52 μM, BTK:2.2 nM, EGFR:3.02 μM, ERB4:0.77 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)
Color	White
Appearance	Solid

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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