Tolebrutinib (Synonyms: SAR442168; PRN2246) |
| Catalog No.GC63232 |
Le tolébrutinib (SAR442168) est un inhibiteur puissant, sélectif, actif par voie orale et pénétrant dans le cerveau de la Bruton tyrosine kinase (BTK), avec des CI50 de 0,4 et 0,7 nM dans les cellules Ramos B et dans les cellules de la microglie HMC, respectivement.
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Cas No.: 1971920-73-6
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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].
[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.
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