Masitinib Inhibitor CAS No. 790299-79-5

Cat. No.	Name	Size	Price
KI1359	Masitinib	10 mg	$144
	Masitinib	25 mg	$272
	Masitinib	200 mg	$1392

Chemical Characteristic

Product Name	Masitinib
Synonyms	AB1010
CAS No.	790299-79-5
Molecular Weight	498.64
Formula	C₂₈H₃₀N₆OS
Chemical Name	N-(4-methyl-3-(4-(pyridin-3-yl)thiazol-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
Smiles	C(=O)(c1ccc(cc1)CN1CCN(CC1)C)Nc1cc(c(cc1)C)Nc1scc(n1)c1cnccc1
Chemical Structure

Biological activities

Masitinib is a potent and selective inhibitor of KIT. The IC50 of masitinib is approximately 200 nM against wild-type human and murine KIT in vitro.^[1] In vitro, Compared to imatinib, masitinib has greater activity and selectivity against KIT and also more strongly inhibits degranulation, cytokine production, and bone marrow mast cell migration. At concentrations of 10, 1.0 and 0.1 µM, masitinib inhibits β-hexosaminidase release by 35, 18 and 7%, respectively, compared to an inhibition of 19, 8 and 2%, respectively for imatinib. Masitinib blocks stem cell factor-induced proliferation and KIT tyrosine phosphorylation in Ba/F3 cells which express human or mouse wild-type KIT. The IC50 of masitinib is 150 nM against KIT tyrosine phosphorylation. Moreover, masitinib also potently inhibits recombinant PDGFR, as well as the intracellular kinase Lyn. However, masitinib potently prevents fibroblast growth factor receptor 3 with a lesser extent. Masitinib is inactive against Flt3 (>10 µM) but moderately inhibits c-Fms in both cell proliferation and recombinant protein kinase assays with IC50 of 1.0 and 1.48 µM, respectively. For a comparison, masitinib weakly inhibits ABL and c-Fms and is inactive against a variety of other tyrosine and serine/threonine kinases.^[2] Administered p.o. masitinib blocks the growth of tumors expressing juxtamembrane-mutated KIT in mice.^[1] In vivo, masitinib inhibits tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant. Masitinib at 30 or 45 mg/kg significantly represses tumour growth following 11 days of treatment compared to placebo, with average tumour volume increases of 355% and 154%. ^[2] In dogs with nonresectable mast cell tumors, masitinib significantly improves survival rate, compared with results for the placebo, with 59 of 95 (62.1%) and 9 of 25 (36.0%) dogs alive at 12 months and 33 of 83 (39.8%) and 3 of 20 (15.0%) dogs alive at 24 months, respectively.^[3]

Protocols

In vitro: Masitinib is practically insoluble in 0.1 M NaOH and n-hexane, slightly soluble in ethanol and propylene glycol, soluble in water, and freely soluble in 0.1 M HCl and dimethylsulfoxide.^[2]

References

[1] Hahn KA, et al. Masitinib is safe and effective for the treatment of canine mast cell tumors. J Vet Intern Med. 2008, 22(6): 1301-1309. [2] Dubreuil P, et al. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PLoS One. 2009, 4(9): e7258. [3] Hahn KA, et al. Evaluation of 12- and 24-month survival rates after treatment with masitinib in dogs with nonresectable mast cell tumors. Am J Vet Res. 2010, 71(11): 1354-1361.

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