SILA-123 (SILA123) is a potent, selective type II FLT3 inhibitor with IC50 of 2.1 nM and 1.0 nM for FLT3-WT and FLT3-ITD respectively.
SILA-123 exhibits promising kinome selectivity against 310 kinases (S score (10) = 0.06).
SILA-123 potently inhibits tumor cells with the FLT3-ITD mutant such as MOLM-13 (IC50 = 0.98 nM) and MV4-11 (IC50 = 0.19 nM), as well as BaF3 cells associated with the FLT3-ITD mutant and point mutations like BaF3-FLT3-ITD-G697R (IC50 = 3.0 nM).
SILA-123 significantly suppressed the tumor growth in MV4-11 (50 mg/kg/d, TGI = 87.3%) and BaF3-FLT3-ITD-G697R (50 mg/kg/d, TGI = 60.0%) cell-inoculated allograft models.
