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Tolebrutinib (Synonyms: SAR442168, PRN2246)

Name: Tolebrutinib
Brand: TargetMol
SKU: T9125
Price: 36 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T9125 Copy Product Info

Purity: 98.82%

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Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

Tolebrutinib

Copy Product Info

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Catalog No. T9125

Synonyms SAR442168, PRN2246

Cas No. 1971920-73-6

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Pack Size	Price	USA Stock	Global Stock
2 mg	$36	In Stock	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$113	In Stock	In Stock
25 mg	$197	In Stock	In Stock
50 mg	$293	In Stock	In Stock
100 mg	$483	In Stock	In Stock
200 mg	$692	-	In Stock
1 mL x 10 mM (in DMSO)	$77	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:98.82%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).
Targets&IC50	BTK:0.4 nM (in Ramos B cells) , BTK:0.7 nM(in HMC microglia cell)
In vitro	PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.?PRN2246 blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells[1].
In vivo	PRN2246 produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[1]
Synonyms	SAR442168, PRN2246

Chemical Properties

Molecular Weight	455.51
Formula	C₂₆H₂₅N₅O₃
Cas No.	1971920-73-6
Smiles	Nc1nccc2n([C@@H]3CCCN(C3)C(=O)C=C)c(=O)n(-c3ccc(Oc4ccccc4)cc3)c12
Relative Density.	1.334 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: 122.5 mg/mL (268.93 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.78 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	2.1953 mL	10.9767 mL	21.9534 mL	109.7671 mL
5 mM	0.4391 mL	2.1953 mL	4.3907 mL	21.9534 mL
10 mM	0.2195 mL	1.0977 mL	2.1953 mL	10.9767 mL
20 mM	0.1098 mL	0.5488 mL	1.0977 mL	5.4884 mL
50 mM	0.0439 mL	0.2195 mL	0.4391 mL	2.1953 mL
100 mM	0.0220 mL	0.1098 mL	0.2195 mL	1.0977 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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