Masitinib (AB-1010) mesylate is a potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays.
Masitinib (AB-1010) also inhibits Lyn, and to a lesser extent, FGFR3, and inhibits KIT gain-of-function mutants V559D (IC50=3.0 nM) and Δ27 mouse mutant (IC50=5 nM).
Masitinib (AB-1010) dose-dependently inhibits SCF-induced cell proliferation in Ba/F3 cells expressing human wild-type KIT (IC50=150 nM); inhibits tumour growth in vivo.
