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CAS No.: 1146699-66-2
Synonyms: BMS-708163
Avagacestat is an inhibitor of γ-secretase Aβ40 and Aβ42 with IC50s of 0.3 nM and 0.27 nM, respectively.
生物活性
靶点 | Amyloid-β 40 IC50:0.3nM | Amyloid-β 42 IC50:0.27nM |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|---|---|---|---|---|
NCT00901498 | Alzheimer's Disease ... more >> Healthy Collapse << | Phase 1 | Completed | - | United States, New Jersey ... more >> Mds Pharma Services (Us) Inc. Neptune, New Jersey, United States, 07753 Collapse << |
NCT00810147 | Alzheimer's Disease | Phase 2 | Completed | - | - |
NCT00828646 | Healthy | Phase 1 | Completed | - | Japan ... more >> Local Institution Yokohama, Kanagawa, Japan, 2320064 Collapse << |
实验方案
技术信息
CAS号 | 1146699-66-2 | 储存条件 |
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分子式 | C20H17ClF4N4O4S | 运输 | 蓝冰 | |||||||||||||
分子量 | 520.89 | 别名 | BMS-708163 | |||||||||||||
溶解度 |
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动物实验配方 |
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Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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CHO cells | - | Function assay | - | Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA, ED50=1.2 nM | 23713656 |
HEK293 cells | - | Function assay | - | Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis, IC50=1.2 nM | 23312944 |
human 786-0 cell | - | Growth inhibition assay | - | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.32173 μM | SANGER |
human BB49-HNC cell | - | Growth inhibition assay | - | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=14.4138 μM | SANGER |
human Calu-6 cell | - | Growth inhibition assay | - | Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=4.96014 μM | SANGER |
human CAPAN-1 cell | - | Growth inhibition assay | - | Inhibition of human CAPAN-1 cell growth in a cell viability assay, IC50=5.17886 μM | SANGER |
human CAS-1 cell | - | Growth inhibition assay | - | Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=13.671 μM | SANGER |
human COLO-668 cell | - | Growth inhibition assay | - | Inhibition of human COLO-668 cell growth in a cell viability assay, IC50=5.40221 μM | SANGER |
human D-502MG cell | - | Growth inhibition assay | - | Inhibition of human D-502MG cell growth in a cell viability assay, IC50=14.9034 μM | SANGER |
human EW-11 cell | - | Growth inhibition assay | - | Inhibition of human EW-11 cell growth in a cell viability assay, IC50=14.8832 μM | SANGER |
human H4 cells | - | Function assay | - | Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cells expressing human APP swedish mutant, IC50=0.225 μM | 22420884 |
human HCT-116 cell | - | Growth inhibition assay | - | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50=18.7965 μM | SANGER |
human HT-1080 cell | - | Growth inhibition assay | - | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=2.48764 μM | SANGER |
human IGR-1 cell | - | Growth inhibition assay | - | Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=1.04778 μM | SANGER |
human IMR32 cell | - | Function assay | 2 h | Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA, IC50=0.13 nM | 23312944 |
human IMR32 cell | - | Function assay | 2 h | Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA, IC50=1.5 nM | 23312944 |
human KINGS-1 cell | - | Growth inhibition assay | - | Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=14.3762 μM | SANGER |
human LCLC-97TM1 cell | - | Growth inhibition assay | - | Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=10.0886 μM | SANGER |
human MDA-MB-157 cell | - | Growth inhibition assay | - | Inhibition of human MDA-MB-157 cell growth in a cell viability assay, IC50=14.2431 μM | SANGER |
human MMAC-SF cell | - | Growth inhibition assay | - | Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50=15.0833 μM | SANGER |
human NCI-H1648 cell | - | Growth inhibition assay | - | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=15.778 μM | SANGER |
human NCI-H23 cell | - | Growth inhibition assay | - | Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50=3.9322 μM | SANGER |
human NCI-H292 cell | - | Growth inhibition assay | - | Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50=15.8806 μM | SANGER |
human NCI-H810 cell | - | Growth inhibition assay | - | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=0.42598 μM | SANGER |
human NMC-G1 cell | - | Growth inhibition assay | - | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=16.6293 μM | SANGER |
human RPMI-2650 cell | - | Growth inhibition assay | - | Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=13.8124 μM | SANGER |
human SAS cell | - | Growth inhibition assay | - | Inhibition of human SAS cell growth in a cell viability assay, IC50=17.7812 μM | SANGER |
human SBC-5 cell | - | Growth inhibition assay | - | Inhibition of human SBC-5 cell growth in a cell viability assay, IC50=19.03 μM | SANGER |
human SK-MEL-3 cell | - | Growth inhibition assay | - | Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=1.49922 μM | SANGER |
human SK-UT-1 cell | - | Growth inhibition assay | - | Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=14.6882 μM | SANGER |
human TE-6 cell | - | Growth inhibition assay | - | Inhibition of human TE-6 cell growth in a cell viability assay, IC50=6.19082 μM | SANGER |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|
NCT00901498 | Alzheimer's Disease ... more >> Healthy Collapse << | Phase 1 | Completed | - | United States, New Jersey ... more >> Mds Pharma Services (Us) Inc. Neptune, New Jersey, United States, 07753 Collapse << |
NCT00810147 | Alzheimer's Disease | Phase 2 | Completed | - | - |
NCT00828646 | Healthy | Phase 1 | Completed | - | Japan ... more >> Local Institution Yokohama, Kanagawa, Japan, 2320064 Collapse << |
NCT00726726 | Alzheimer Disease | Phase 1 | Completed | - | United States, New Jersey ... more >> Bristol-Myers Squibb Clinical Pharmacology Unit Hamilton, New Jersey, United States, 08690 Collapse << |
NCT01079819 | Alzheimer's Disease | Phase 1 | Completed | - | United States, California ... more >> West Coast Clinical Trials, Llc Cypress, California, United States, 90630 California Clinical Trials Medical Group Glendale, California, United States, 91206 United States, New Jersey Iberica Clinical Research Center Eatontown, New Jersey, United States, 07724 Collapse << |
NCT00979316 | Alzheimer Disease | Phase 1 | Completed | - | United States, Arizona ... more >> Mds Pharma Services (Us), Inc Tempe, Arizona, United States, 85283 Collapse << |
NCT01002079 | Alzheimer Disease | Phase 1 | Completed | - | India ... more >> Local Institution Bangalore, India, 560100 Collapse << |
NCT01454115 | Alzheimer's Disease | Phase 1 | Completed | - | - |
NCT01057030 | Alzheimer Disease | Phase 1 | Completed | - | United States, California ... more >> California Clinical Trials Medical Group Glendale, California, United States, 91206 Collapse << |
NCT00860275 | Alzheimer Disease | Phase 1 | Completed | - | United States, Texas ... more >> Ppd Development, Lp Austin, Texas, United States, 78744 Collapse << |
NCT01039194 | Alzheimer Disease | Phase 1 | Completed | - | United States, Maryland ... more >> Parexel International - Baltimore Epcu Baltimore, Maryland, United States, 21225 Collapse << |
NCT00890890 | Alzheimer's Disease | Phase 2 | Terminated | - | - |
NCT01042314 | Alzheimer Disease | Phase 1 | Completed | - | United States, Maryland ... more >> Parexel International - Baltimore Epcu Baltimore, Maryland, United States, 21225 Collapse << |
靶点 | Description | IC50 |
---|---|---|
Amyloid-β 40 | IC50:0.3nM | |
Amyloid-β 42 | IC50:0.27nM |
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