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Tolebrutinib
Catalog No. T9125Cas No. 1971920-73-6
Alias SAR442168, PRN2246
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).
Tolebrutinib
Catalog No. T9125Alias SAR442168, PRN2246Cas No. 1971920-73-6
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 | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $36 | In Stock | |
| 5 mg | $68 | In Stock | |
| 10 mg | $113 | In Stock | |
| 25 mg | $197 | In Stock | |
| 50 mg | $293 | In Stock | |
| 100 mg | $483 | In Stock | |
| 200 mg | $692 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $77 | In Stock |
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Atuzabrutinib
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Edralbrutinib
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Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity used in treating tumors, immune system disorders, and blood and lymphatic system disorders. Additionally, Edralbrutinib is studied for its efficacy in membranous glomerulonephritis and optic neuromyelitis optica.
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Purity:98.82%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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] |
| Alias | SAR442168, PRN2246 |
| Molecular Weight | 455.51 |
| Formula | C26H25N5O3 |
| Cas No. | 1971920-73-6 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (219.53 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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