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Masitinib is a potent inhibitor of the tyrosine kinase receptor colony-stimulating factor 1R (CSF-1R) (IC50 = 90 nM). It is also an NLRP3 inflammasome activator. Masitinib additionally inhibits the proteolytic activity of SARS-CoV-2 main protease (Mpro) and blocks viral replication, as well as acting as a PDGFRα/β inhibitor. In vivo, Masitinib ameliorates cognitive impairment in transgenic mice model of Alzheimer's disease, and slows disease progression in a rat model of amyotrophic lateral sclerosis (ALS). Orally bioavailable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 498.64. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.01 mL||10.03 mL||20.05 mL|
|5 mM||0.4 mL||2.01 mL||4.01 mL|
|10 mM||0.2 mL||1 mL||2.01 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Martínez-Ortega et al (2021) In silico characterization of Masitinib interaction with SARS-CoV-2 main protease. ChemMedChem. 16 2339 PMID: 34142459
Li et al (2020) Effects of chronic Masitinib treatment in APPswe/PSEN1dE9 transgenic mice modeling Alzheimer's disease. J.Alzheimers.Dis. 76 1339 PMID: 32623401
Trias et al (2016) Post-paralysis tyrosine kinase inhibition with masitinib abrogates neuroinflammation and slows disease progression in inherited amyotrophic lateral sclerosis. J.Neuroinflammation 13 177 PMID: 27400786
Ettcheto et al (2021) Masitinib for the treatment of Alzheimer's disease. Neurodegener.Dis.Manag. 11 263 PMID: 34412534
Drayman et al (2021) Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2. Science 373 931 PMID: 34285133
If you know of a relevant reference for Masitinib, please let us know.
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