Avagacestat acts as a γ-secretase inhibitor allowing for treatment of ALzheimer’s disease. On addition it has seen uses targeting embryonic signaling pathways, which control stem cell and cellular development process in cancer therapy.
This orally bioavailable, selective protease inhibitor (FW = 520.88 g/mol;
CAS 1146699-66-2; Solubility: 100 mg/mL DMSO; <1 mg/mL Water;
Formulation for Animal Studies: 99% PEG-400, 1% Tween-80 (in rats) or
94% labrafil-1944, 5% ethanol, 1% tween-80 (in dogs) ), known as
Avagacestat and (2R) -2- (N- (2-fluoro-4- (1,2,4-oxadiazol-3-yl) benzyl) -4-
chlorophenylsulfonamido) -5,5,5-trifluoropentanamide, targets γ-secretase
(GS), thereby inhibiting the formation of Aβ40 and Aβ42, with IC50 values
of 0.3 nM and 0.27 nM, respectively.