Tolebrutinib

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) [1][2].

Product Specifications

CAS Number

[1971920-73-6]

Product Name Alternative

SAR442168; PRN2246

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Btk

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/tolebrutinib.html

Purity

99.79

Solubility

DMSO : 87.5 mg/mL (ultrasonic)

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

Molecular Formula

C26H25N5O3

Molecular Weight

455.51

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.