Masitinib

Key Product Details

Product Description

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 (M^pro) 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.

Product Specifications for Masitinib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Masitinib

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.01 mL	10.03 mL	20.05 mL
5 mM	0.40 mL	2.01 mL	4.01 mL
10 mM	0.20 mL	1.00 mL	2.01 mL
50 mM	0.04 mL	0.20 mL	0.40 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Drayman Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2. Science 2021 PMID: 34285133
• Ettcheto Masitinib for the treatment of Alzheimer's disease. Neurodegener.Dis.Manag. 2021 PMID: 34412534
• Li Effects of chronic Masitinib treatment in APPswe/PSEN1dE9 transgenic mice modeling Alzheimer's disease. J.Alzheimers.Dis. 2020 PMID: 32623401
• Trias Post-paralysis tyrosine kinase inhibition with masitinib abrogates neuroinflammation and slows disease progression in inherited amyotrophic lateral sclerosis. J.Neuroinflammation 2016 PMID: 27400786
• Martínez-Ortega In silico characterization of Masitinib interaction with SARS-CoV-2 main protease. ChemMedChem. 2021 PMID: 34142459

Product Documents for Masitinib