Masitinib

Name: Masitinib
Brand: Tocris Bioscience
SKU: 7705

Tocris Bioscience, part of Bio-Techne | Catalog # 7705

COA / SDS

Potent colony-stimulating factor 1 receptor (CSF-1R) tyroine kinase inhibitor

Key Product Details

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)
Molecular Weight:	498.64

View Full Technical Details for Masitinib

Technical Data
Citations

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 (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.

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 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.

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

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References for Masitinib

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