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Masitinib (AB1010)

Tyrosine kinase inhibitor, potent and selective

Masitinib (AB1010)

Catalog No. A2942
Size Price Stock Qty
5mg $50.00 In stock
25mg $100.00 In stock
100mg $300.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Masitinib (AB1010)

Biological Activity

Description Masitinib is a potent and selective inhibitor of tyrosine kinases with IC50 values of 200 nM, 540 nM and 800 nM for KIT, PDGFRα and PDGFRβ, respectively.
Targets KIT PDGFRα PDGFRβ      
IC50 200 nM 540 nM 800 nM      

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Chemical Properties

Cas No. 790299-79-5 SDF Download SDF
Chemical Name 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide
Canonical SMILES CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC(=CS4)C5=CN=CC=C5
Formula C28H30N6OS M.Wt 498.64
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

The stem cell factor receptor (KIT) is a therapeutic target for the cancer, mastocytosis, and inflammatory diseases treatment. Masitinib (AB1010) is a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.
In vitro: Masitinib potently inhibited the intracellular kinase Lyn and recombinant PDGFR as well as fibroblast growth factor receptor 3. Moreover, masitinib showed weak inhibition of ABL and c-Fms and was inactive against a variety of other tyrosine and serine/threonine kinases. These findings suggest that Masitinib (AB1010) will exhibit a better safety profile than other tyrosine kinase inhibitors; in fact, masitinib-induced genotoxicity or cardiotoxicity has not been observed in animal so far [1].
In vivo: In vivo, masitinib blocked tumour growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant. We found that tumour growth was blocked following 5 days of treatment with masitinib. After withdrawal of masitinib treatment after day 5, tumour growth was once again evident [1].
Clinical trial: A Phase II study of oral masitinib mesilate in imatinib-naïve patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). Thirty patients were enrolled with a median follow-up of 34 months. Masitinib appears to be effective as a first-line treatment of advanced GIST with comparable results to imatinib in terms of safety and response. PFS and OS results data show promise that masitinib may provide sustainable benefits [2].
Reference:
[1] Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W, Voisset E, Arock M, Auclair C, Leventhal PS, Mansfield CD, Moussy A, Hermine O. Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT. PLoS One. 2009;4(9):e7258.
[2] Sylvie Bonvalot , Alain Moussy , Jean-Pierre Kinet , et al. Phase II study of oral masitinib mesilate in imatinib-naïve patients with locally advanced or metastatic gastro-intestinal stromal tumour (GIST). European Journal of Cancer. 2010(46): 1344-1351