|
Biological Activity:
A potent oral tyrosine kinase inhibitor, targeting c-KIT and PDGFR (IC50: 150, 300 and 50 nM for KIT, PDGFRα and PDGFRβ respectively); To a lesser extend, it inhibits FGFR3 (IC50: 5500 nM); oncology drug under clinical trial.
References:
P Dubreuil et al. Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT. Plos ONE 2009, 4(9), e7258. [online]
BN Bui, et al. Preliminary efficacy and safety results of masitinib administered, front line in patients with advanced GIST. A phase II study. J. Clin. Onco. 2007, 25(18S), 10025. [abstract]
G Giamas et al. Protein kinases as targets for cancer treatment. Pharmacogenomics. 2007, 8(8), 1005-1016. [abstract]
KA Hahn et al. Masitinib is safe and effective for the treatment of canine mast cell tumors. J. Vet. Intern. Med. 2008, 22(6), 1301-1309. [abstract]
Chemical Name: 4-(4-Methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-phenyl]-benzamide methanesulfonate
| 
