| 英文名称: | | pf-03084014 hydrobromide | | (2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-n-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1h-imidazol-4-yl]-pentanamide hydrobromide | | pf 3084014 hydrobromide | | nirogacestat | | pf 03084014 hydrobromide | | pf-3084014 hydrobromide |
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| 用途: | Nirogacestat (PF-03084014, PF-3084014) 是一种选择性gamma-secretase抑制剂，在无细胞试验中IC50为6.2 nM。Phase 2。PF-03084014 inhibits Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1with IC50 of 13.3 nM. PF-03084014 downregulates Notch target genes Hes-1, and cMyc expression in HPB-ALL cells with IC50 of <1 nM and 10 nM, respectively. PF-03084014 inhibits cell growth of a subset of human T-ALL cell lines (HPB-ALL, DND-41, TALL-1,and Sup-T1) through induction of cell cycle arrest and apoptosis with IC50s of 30-100 nM. [1]PF-03084014 reduces proliferation of HUVECs with IC50 of 0.5 μM, and decreases the lumen formation with an IC50 value of 50 nM. PF-03084014 (1 μM) has no antiproliferative effect in MX1 cells; however, it inhibits migration by 95%. [2] |
