Avagacestat
产品说明书
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同义名 : | BMS-708163 |
| CAS号 : | 1146699-66-2 | |
| 货号 : | A329302 | |
| 分子式 : | C20H17ClF4N4O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 520.885 | |
| MDL号 : | MFCD13195458 | |
| 存储条件： |
Pure form Sealed in dry,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(201.58 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear PO 0.5% CMC-Na 85 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Avagacestat (BMS-708163) has a demonstrated IC50 of 58±23 nM for inhibiting Notch processing, which is weaker compared to its potency for inhibiting APP cleavage[1]. In cell culture studies, Avagacestat (BMS-708163) at a concentration of 10 µM when combined with gefitinib, significantly reduces colony growth in PC9/AB2 cells. This combination treatment not only enhances the expression of active caspase 3 and PARP but also diminishes Ki-67 expression, indicating increased apoptosis and enhanced cell cycle arrest at the G1 phase. Furthermore, Avagacestat effectively downregulates the expression of Notch1, HES1, PI3K, and Akt in these cells[3]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| 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 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| 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 ... 展开 >> Healthy 收起 << | Phase 1 | Completed | - | United States, New Jersey ... 展开 >> Mds Pharma Services (Us) Inc. Neptune, New Jersey, United States, 07753 收起 << |
| NCT00810147 | Alzheimer's Disease | Phase 2 | Completed | - | - |
| NCT00828646 | Healthy | Phase 1 | Completed | - | Japan ... 展开 >> Local Institution Yokohama, Kanagawa, Japan, 2320064 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.92mL 0.38mL 0.19mL |
9.60mL 1.92mL 0.96mL |
19.20mL 3.84mL 1.92mL |
| 参考文献 |
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