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Tirabrutinib hydrochloride

Name: Tirabrutinib hydrochloride
Brand: TargetMol
SKU: T12311
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12311Cas No. 1439901-97-9

Alias ONO-4059 (hydrochloride), GS-4059 (hydrochloride)

Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].

Tirabrutinib hydrochloride

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Purity: 99.95%

Catalog No. T12311Alias ONO-4059 (hydrochloride), GS-4059 (hydrochloride)Cas No. 1439901-97-9

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$43	In Stock	In Stock
10 mg	$71	In Stock	In Stock
25 mg	$126	In Stock	In Stock
50 mg	$207	-	In Stock
100 mg	$369	-	In Stock
1 mL x 10 mM (in DMSO)	$48	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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Purity:99.95%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].
Targets&IC50	TEC:48 nM, EGFR:3.02 μM, BTK:2.2 nM, BLK:0.3 μM, BMX?kinase:6 nM, ERB4:0.77 μM, TXK:92 nM, ERBB2:7.31 μM, JAK3:5.52 μM
In vitro	METHODS: Tirabrutinib hydrochloride (0.1-1000 nM or 0.001-100 nM; 72 h) was used to treat DLBCL cell lines SU-DHL-6 and OCI-LY10 to observe the anti-tumor effect on cells. RESULTS The IC50 values of Tirabrutinib hydrochloride against SU-DHL-6 and OCI-LY10 cell lines were 9.127 μM, and 17.10 μM.[1]
In vivo	Parental TMD8 mice were treated with tirabrutinib (6, 20 mg/kg; p.o.) to confirm whether tirabrutinib remains active in vivo. RESULTS 0.012% of tirabrutinib resulted in tumor remission in mice. [2]
Synonyms	ONO-4059 (hydrochloride), GS-4059 (hydrochloride)

Chemical Properties

Molecular Weight	490.94
Formula	C₂₅H₂₃ClN₆O₃
Cas No.	1439901-97-9
Smiles	Cl.CC#CC(=O)N1CC[C@H](C1)n1c2ncnc(N)c2n(-c2ccc(Oc3ccccc3)cc2)c1=O
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 95 mg/mL (193.51 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.07 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	2.0369 mL	10.1845 mL	20.3691 mL	101.8454 mL
5 mM	0.4074 mL	2.0369 mL	4.0738 mL	20.3691 mL
10 mM	0.2037 mL	1.0185 mL	2.0369 mL	10.1845 mL
20 mM	0.1018 mL	0.5092 mL	1.0185 mL	5.0923 mL
50 mM	0.0407 mL	0.2037 mL	0.4074 mL	2.0369 mL
100 mM	0.0204 mL	0.1018 mL	0.2037 mL	1.0185 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