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Tolebrutinib

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

🥰Excellent

Catalog No. T9125Cas No. 1971920-73-6

Alias SAR442168, PRN2246

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

🥰Excellent

Purity: 98.82%

Catalog No. T9125Alias SAR442168, PRN2246Cas No. 1971920-73-6

Pack Size	Price	USA Warehouse	Global Warehouse
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

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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:98.82%

Resource Download

COA HNMR HPLC

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: 100 mg/mL (219.53 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

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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