Home Angiogenesis BTK inhibitor Tolebrutinib For research use only.

Tolebrutinib

Synonyms: SAR442168, PRN2246

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.

Tolebrutinib Chemical Structure

Tolebrutinib Chemical Structure

CAS No. 1971920-73-6

Purity & Quality Control

Tolebrutinib Related Products

Signaling Pathway

BTK Signaling Pathways

BTK Signaling Pathway

Biological Activity

Description 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.
Targets
BTK [1]
(in Ramos B cell)		 BTK [1]
(in HMC microglia cells)
0.4 nM 0.7 nM
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

Chemical Information & Solubility

Molecular Weight 455.51 Formula

C₂₆H₂₅N₅O₃
CAS No. 1971920-73-6 SDF --
Smiles NC1=NC=CC2=C1N(C(=O)N2C3CCCN(C3)C(=O)C=C)C4=CC=C(OC5=CC=CC=C5)C=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (199.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


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In vivo
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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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