Crenigacestat
产品说明书
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同义名 : | LY3039478 |
| CAS号 : | 1421438-81-4 | |
| 货号 : | A236352 | |
| 分子式 : | C22H23F3N4O4 | |
| 纯度 : | 98%+ | |
| 分子量 : | 464.44 | |
| MDL号 : | MFCD26142650 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | LY3039478 is a potent Notch-1 intracellular domain (N1ICD) cleavage inhibitor with IC50 value of 0.41nM in SAR assays[1]. It inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment, and also resulted in the induction of apoptosis in a Notch-dependent xenograft model[2]. LY3039478 at concentration of 1μM and 10μM significantly inhibited the growth of Caki and 769-P, with decreased expression of Myc and Cyclin A1, two protein driven by Notch. G0/G1 cell cycle arrest could also be observed. Oral administration of LY3039478, 3 days per week, led a significant increase of survival and delayed tumor growth of immunodeficient NSG mice xenografted with 769-P CCRCC 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 |
| A2780 cells | Function assay | 24 h | Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A2780 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA, IC50=0.00103 μM | 24900678 | |
| A375 cells | Function assay | 24 h | Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A375 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA, IC50=0.00048 μM | 24900678 | |
| BxPC3 cells | Function assay | 24 h | Inhibition of gamma-secretase mediated cleavage of Notch 1 in human BxPC3 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA, IC50=0.00039 μM | 24900678 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.22mL |
10.77mL 2.15mL 1.08mL |
21.53mL 4.31mL 2.15mL |
| 参考文献 |
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