PF-3084014 is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.
CAS：1290543-63-3
分子式：C27H41F2N5O
分子量：489.64
纯度：98%
存储：Store at -20°C

Background:

PF-3084014 is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.

The IC50 of PF-03084014 for γ-secretase enzyme inhibition in cell-free assay for Aβ production using detergent solubilized membranes derived from HeLa cells is determined to be 6.2 nM. When tested for inhibition of Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1, the cell IC50 is determined to be 13.3 nM. PF-03084014 causes a significant increase in caspase-3 activities in HPB-ALL and TALL-1 cells as well as an induction of cleaved PARP and cleaved caspase-3 after a 7-day treatment[1].

PF-03084014 shows robust antitumor activity in this model on 14-day twice daily dosing. Tumor growth inhibition is dose dependent, with maximal tumor growth inhibition of