Tolebrutinib (Synonyms: SAR442168; PRN2246)

Name: Tolebrutinib
Brand: MedChemExpress
SKU: HY-109192
Rating: 5.0 (4 reviews)

Cat. No.: HY-109192 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC₅₀s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

For research use only. We do not sell to patients.

Tolebrutinib Chemical Structure

CAS No. : 1971920-73-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 95	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 95	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 365	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 585	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Tolebrutinib

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Description

IC₅₀ & Target

IC50: 0.7 nM (BTK; in HMC microglia cells)^[2]

In Vitro

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^[2].
? PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC₅₀ of 157 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PRN2246 (1-5 mg/kg; p.o. q.d. for 28 d) produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

455.51

Formula

C₂₆H₂₅N₅O₃

CAS No.

1971920-73-6

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1[C@H]2CN(C(C=C)=O)CCC2)N(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C1C=CN=C5N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (219.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1953 mL	10.9767 mL	21.9534 mL
5 mM	0.4391 mL	2.1953 mL	4.3907 mL
10 mM	0.2195 mL	1.0977 mL	2.1953 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (257 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Dahl K, et, al. Radiosynthesis of a Bruton's tyrosine kinase inhibitor, [ 11 C]Tolebrutinib, via palladium-NiXantphos-mediated carbonylation. J Labelled Comp Radiopharm. 2020 Sep;63(11):482-487. [Content Brief]

[2]. Francesco MR, et, al. PRN2246, a potent and selective blood brain barrier penetrating BTK inhibitor, exhibits efficacy in central nervous system immunity. Multiple Sclerosis Journal. 2017;Poster Session 2:P989.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1953 mL	10.9767 mL	21.9534 mL	54.8835 mL
	5 mM	0.4391 mL	2.1953 mL	4.3907 mL	10.9767 mL
	10 mM	0.2195 mL	1.0977 mL	2.1953 mL	5.4884 mL
	15 mM	0.1464 mL	0.7318 mL	1.4636 mL	3.6589 mL
	20 mM	0.1098 mL	0.5488 mL	1.0977 mL	2.7442 mL
	25 mM	0.0878 mL	0.4391 mL	0.8781 mL	2.1953 mL
	30 mM	0.0732 mL	0.3659 mL	0.7318 mL	1.8295 mL
	40 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3721 mL
	50 mM	0.0439 mL	0.2195 mL	0.4391 mL	1.0977 mL
	60 mM	0.0366 mL	0.1829 mL	0.3659 mL	0.9147 mL
	80 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6860 mL
	100 mM	0.0220 mL	0.1098 mL	0.2195 mL	0.5488 mL

Tolebrutinib Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tolebrutinib (Synonyms: SAR442168; PRN2246)

Customer Review

Tolebrutinib Related Antibodies

4 Publications Citing Use of MCE Tolebrutinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Tolebrutinib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Tolebrutinib Related Classifications

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