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Masitinib

Cat. No. 7705 Submit a Review Datasheet / COA / SDS
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Description: Potent colony-stimulating factor 1 receptor (CSF-1R) tyroine kinase inhibitor
Chemical Name: 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-thiazolyl]amino]phenyl]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Masitinib

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.

Technical Data for Masitinib

M. Wt 498.64
Formula C28H30N6OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 790299-79-5
PubChem ID 10074640
InChI Key WJEOLQLKVOPQFV-UHFFFAOYSA-N
Smiles O=C(NC1=CC=C(C(=C1)NC2=NC(=CS2)C=3C=NC=CC3)C)C4=CC=C(C=C4)CN5CCN(C)CC5

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.

Solubility Data for Masitinib

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.86 100
ethanol 4.99 10

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for Masitinib

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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Citations for Masitinib

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