NCIt definition : A small-molecule gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic
activity. Upon intravenous administration, osugacestat binds to GS and blocks activation
of Notch receptors, which may inhibit the proliferation of tumor cells with an overly-active
Notch pathway. The integral membrane protein GS is a multi-subunit protease complex
that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues
within their transmembrane domains that lead to their activation. Overactivation of
the Notch signaling pathway, often triggered by activating mutations, has been correlated
with increased cellular proliferation and poor prognosis in certain tumor types.;
UNII : DRL23N424R;
CAS number : 1401066-79-2;
Molecule name : AL 101; BMS-906024; AL-101; BM-0018;
Semantic type(s)