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Tolebrutinib BTK inhibitor

Name: Tolebrutinib
Brand: Selleck Chemicals
SKU: E0041
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E0041

Tolebrutinib is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with IC50s of 0.4 nM and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively.

Chemical Structure

Molecular Weight: 455.51

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Quality Control

Batch: Purity: 99.33%

99.33

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other BTK Products	Catadegbrutinib (BGB-16673) Spebrutinib (AVL-292) tirabrutinib(ONO-4059) hydrochloride CGI1746 LFM-A13 CNX-774 BMS-935177 Fenebrutinib (GDC-0853) Branebrutinib (BMS-986195) Evobrutinib

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.500mg/ml (3.29mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.370mg/ml (0.81mM)

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	455.51	Formula	C₂₆H₂₅N₅O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1971920-73-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SAR442168, PRN2246			Smiles	NC1=NC=CC2=C1N(C(=O)N2C3CCCN(C3)C(=O)C=C)C4=CC=C(OC5=CC=CC=C5)C=C4

Mechanism of Action

Targets/IC₅₀/Ki	BTK (in Ramos B cell) 0.4 nM BTK (in HMC microglia cells) 0.7 nM

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05283915	Completed	Hepatic Function Abnormal	Sanofi	March 18 2022	Phase 1
NCT05282030	Completed	Renal Impairment	Sanofi	March 23 2022	Phase 1
NCT04742400	Active not recruiting	Multiple Sclerosis	National Institute of Neurological Disorders and Stroke (NINDS)\|National Institutes of Health Clinical Center (CC)	April 15 2021	Phase 2
NCT06106074	Completed	Multiple Sclerosis	Sanofi	August 10 2020	Phase 1
NCT06064539	Completed	Multiple Sclerosis	Sanofi	May 18 2020	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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