Nirogacestat (PF-03084014, PF-3084014), ≥99.9%,Nirogacestat (PF-03084014, PF-3084014)
产品编号:西域试剂-WR353122| CAS NO:1290543-63-3| MDL NO:MFCD19980705| 分子式:C27H41F2N5O| 分子量:489.64
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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. 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%. |
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储存条件: | -20℃ |
颜色: | 粉末 |
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