Tolebrutinib

1971920-73-6

455.51

DMSO : 100 mg/mL (ultrasonic)

Protein Tyrosine Kinase/RTK

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]. 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 FcepsilonR and FcgammaR, repectively) of immune cells^[2].
PRN2246 inhibits microglial FcgammaR activation through durable occupancy of BTK, with an IC₅₀ of 157 nM^[2]. 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].