| 中文名称: | ABL127 | ||||
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| 英文名称: | ABL127 | ||||
| 别名: | (3R)-Dimethyl 3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine-1,2-dicarboxylate | ||||
| CAS No: | 1073529-41-5 | 分子式: | C17H20N2O5 | 分子量: | 332.35 |
| CAS No: | 1073529-41-5 | ||||
| 分子式: | C17H20N2O5 | ||||
| 分子量: | 332.35 | ||||
基本信息
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产品编号： |
A12825 |
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产品名称： |
ABL127 |
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CAS: |
1073529-41-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
332.35 |
-20℃ |
一个月 |
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化学名： |
(3R)-Dimethyl3-cyclopentyl-4-oxo-3-phenyl-1,2-diazetidine-1,2-dicarboxylate |
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生物活性
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产品描述 |
一个有选择且共价的蛋白质甲基酯酶 1 (PME-1) 抑制剂，在 HEK293T 和 MDA-MB-231 细胞中的 IC50 值分别为 6.4 和 4.2nM。 |
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靶点 |
IC50: 6.4nM (PME-1 in HEK293T), 4.2nM (PME-1 in MDA-MB-231) |
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体外研究 |
Three described PME-1 inhibitors are tested in this assay and a thermal shift with 100μM ABL127 is detected. Using 25 or 50μM ABL127 also shows a shift in protein melting temperature. It is found that treatment of Ishikawa cells with ABL127 and AMZ-30 significantly decreases cell proliferation similarly to depletion of PME-1 with shRNA. It is also found that treatment of ECC-1 cells with ABL127 or AMZ-30 affects cell invasion in a dose-dependent manner. The treatment of EC cells with ABL127 leads to a significant ~45 % increase in protein phosphatase 2A (PP2A) activity, while treatment with AMZ-30 leads to a modest ~10 % increase in PP2A activity |
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体内研究 |
No significant decrease in tumor burden can be assessed in these pilot studies. Gel-based profiles indicate that brain PME1 is inactivated by ABL127, but overlapping serine hydrolase activities preclude a confident assessment of the extent of inactivation |
推荐实验方法(仅供参考)
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Kinase Assay |
Human PME-1 protein lacking the last three amino acids (PME-1des3) is purified from Sf9 cells. The assay is completed by first conducting a 10 min pre-incubation of 1μM PME-1des3 with 100μM ABL127, 100μM AMZ-30, 100μM EHT, or vehicle (0.05 % DMSO) in the presence of SYBR Orange (1:1000, v/v) at 37°C in 1× NEB buffer 2 (50mM NaCl, 10mM Tris-HCl, 10mM MgCl2, 1mM DTT, pH 7.9 at 25 °C); a thermal gradient is performed increasing temperature by 2°C per minute increments from 37 to 95°C, and fluorescence (492 to 610nM) is acquired on a thermal cycler |
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Cell Assay |
Cells are subjected to 5 μg/mL puromycin selection for 10 to 14 days and are clonally expanded. Validated clones are incubated with media and compounds (including ABL127) for the indicated times for phenotypic assays |
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Animal Administration |
ECC-1 cells are subcutaneously inoculated into the flanks of female SCID mice and are allowed to grow until tumors reached ~400mM3 . A single intratumoral dose of ABL127 diluted in 10% DMSO/PBS is administered. The highest concentration tested is 5 mg/kg of ABL127 due to poor solubility of the compound |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
