Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 106.00 | |
5 mg | In stock | $ 263.00 | |
10 mg | In stock | $ 396.00 | |
25 mg | In stock | $ 753.00 | |
50 mg | In stock | $ 1,120.00 | |
100 mg | In stock | $ 1,670.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 363.00 |
Description | Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS). |
Targets&IC50 | BTK:0.4 nM (in Ramos B cells) , BTK:0.7 nM(in HMC microglia cell) |
In vitro | PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.?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[1]. |
In vivo | PRN2246 produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[1] |
Synonyms | PRN2246, SAR442168 |
Molecular Weight | 455.51 |
Formula | C26H25N5O3 |
CAS No. | 1971920-73-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (219.53 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Tolebrutinib 1971920-73-6 Angiogenesis Tyrosine Kinase/Adaptors BTK multiple PRN 2246 inhibit Bruton tyrosine kinase sclerosis Bruton kinase SAR-442168 tyrosine PRN2246 Inhibitor SAR442168 Btk PRN-2246 SAR 442168 inhibitor