Catalog No.: PC-49410Not For Human Use, Lab Use Only.
Nirogacestat (PF-03084014) is a potent, noncompetitive, and selective gamma-secretase inhibitor, reduces amyloid-beta (Abeta) production with in vitro IC50 of 1.2 nM (whole-cell assay) to 6.2 nM (cell-free assay).
Nirogacestat (PF-03084014) is a potent, noncompetitive, and selective gamma-secretase inhibitor, reduces amyloid-beta (Abeta) production with in vitro IC50 of 1.2 nM (whole-cell assay) to 6.2 nM (cell-free assay).
PF-03084014 inhibits Notch-related T- and B-cell maturation in an in vitro thymocyte assay with an EC(50) of 2.1 uM.
PF-03084014 inhibited gamma-secretase activity was shown by the reduction of endogenous Notch intracellular domain (NICD) levels and by the downregulation of Notch target genes Hes-1 and cMyc in the T-cell acute lymphoblastic leukemia (T-ALL) cell line HPB-ALL.
PF-03084014 caused cell growth inhibition of several T-ALL cell lines via cell cycle arrest and induction of apoptosis.
PF-03084014 treatment also resulted in robust NICD reduction in HBP-ALL xenograft models, exhibited broad antitumor efficacy in Notch-dependent models.
