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Tolebrutinib
🥰Excellent
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
🥰Excellent
Purity: 98.82%
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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View MoreInhibitors Related to "Tolebrutinib"
Ibrutinib
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Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
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CitedOrelabrutinib
ICP-022
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Orelabrutinib (ICP-022) is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
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(±)-Zanubrutinib
(±)-BGB-3111
TQ00391633350-06-7
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, orally available Bruton's tyrosine kinase (Btk) inhibitor, exhibiting superior oral bioavailability, higher exposure, and more complete target inhibition.
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IBT6A
T106251022150-12-4
IBT6A, an impurity of Ibrutinib, is a Btk inhibitor (IC50: 0.5 nM) that can be utilized in the synthesis of IBT6A Ibrutinib dimer and IBT6A adduct.
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JAK3/BTK-IN-1
T98142674036-91-8In house
JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.
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Atuzabrutinib
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evobrutinib
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Evobrutinib(M2951) , also known as M-2951 and MSC-2364447C, is a highly selective inhibitor of the Bruton's tyrosine kinase (BTK), which is important in the development and functioning of various immune cells including B -lymphocytes and macrophages. PreClinical research suggests it may be therapeutically useful in certain autoimmune diseases.
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CGI1746 is a potent and highly selective small-molecule Btk inhibitor with IC50 of 1.9 nM.
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Edralbrutinib
TG-1701
T632721858206-58-2In house
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.
- $197
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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 |
| Smiles | Nc1nccc2n([C@@H]3CCCN(C3)C(=O)C=C)c(=O)n(-c3ccc(Oc4ccccc4)cc3)c12 |
| Relative Density. | 1.334 g/cm3 (Predicted) |
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 | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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