A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 that competes against SAM for MAT2A binding and is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM synthesis both in cell-free assays (IC50 = 2.1uM) and in LS174T colorectal cancer (CRC) cultures (3uM). FIDAS-5 at 3uM is shown to completely inhibit the proliferation of LS174T for up to 7 d in vitro and effectively suppress HT29 CRC tumor expansion in mice in vivo (20mg/kg/day p.o.).
Storage and Stability:May be stored at 4°C. Stable for 6 months after receipt. Reconstitute with DMSO. Aliquot and store at -20°C. Stable for 3 months. Hygroscopic and light sensitive. Store under inert gas.