| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.7 nM (BTK; in HMC microglia cells) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| 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]. | ||||||||||||
| Name | Tolebrutinib | ||||||||||||
| CAS | 1971920-73-6 | ||||||||||||
| Formula | C26H25N5O3 | ||||||||||||
| Molar Mass | 455.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Tolebrutinib
CAS: 1971920-73-6 F: C26H25N5O3 W: 455.51
Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (
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