| 中文名称: | Cambinol | ||||
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| 英文名称: | Cambinol | ||||
| 别名: | 5-[(2-羟基萘-1-基)甲基]-6-苯基-2-硫代-2,3-二氢嘧啶-4(1H)-酮 5-((2-hydroxynaphthalen-1-yl)methyl)-6-phenyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one | ||||
| CAS No: | 14513-15-6 | 分子式: | C21H16N2O2S | 分子量: | 360.43 |
| CAS No: | 14513-15-6 | ||||
| 分子式: | C21H16N2O2S | ||||
| 分子量: | 360.43 | ||||
| EINEC: | 112546 | ||||
| EINEC: | 112546 | ||||
基本信息
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产品编号：C10816 |
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产品名称：Cambinol |
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CAS: |
14513-15-6 |
储存条件 |
粉末 |
-20℃（避光） |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
360.43 |
-20℃ |
一个月 |
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化学名： |
5-((2-hydroxynaphthalen-1-yl)methyl)-6-phenyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one |
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Solubility (25°C) |
体外 |
DMSO |
21mg/mL (58.26mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内 |
现配现用 |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.7745mL |
13.8723mL |
27.7446mL |
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5mM |
0.5549mL |
2.7745mL |
5.5489mL |
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10mM |
0.2774mL |
1.3872mL |
2.7745mL |
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50mM |
0.0555mL |
0.2774mL |
0.5549mL |
生物活性
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产品描述 |
一种 SIRT1 和 SIRT2 的抑制剂，IC50 值分别为 56μM 和 59μM。 |
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靶点/IC50 |
SIRT1 56μM (IC50) |
SIRT2 59μM (IC50) |
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体外研究 |
Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. Inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induces apoptosis, which is accompanied by hyperacetylation of BCL6 and p53. Cambinol has only weak inhibitory activity against SIRT5 (42% inhibition at 300μM) and no activity against SIRT3. |
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体内研究 |
Cambinol is well tolerated in mice (100mg/kg) and inhibits growth of Burkitt lymphoma xenografts. No significant weight loss occurs in cambinol-treated animals relative to controls. Inhibitors of NAD-dependent deacetylases may constitute novel anticancer agents . |
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推荐实验方法(仅供参考)
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细胞实验： |
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Cell Assay |
The reporter construct with or without varying amounts of GAL4-BCL6 expression plasmid are introduced into NCI-H460 cells using calcium phosphate method. A plasmid containing cytomegalovirus (CMV)-driven β-galactosidase reporter (50ng) is cotransfected to control for transfection efficiency. Sixteen hours after transfection, cells are treated with 100μM cambinol of DMSO (control) for 24 hours and the luciferase and β-galactosidase activity is measured. |
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动物实验: |
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Animal Administration |
Mice: Cambinolat the dose of 100mg/kg, or vehicle are administered i.v. through tail vein injection or i.p. daily from day 5 to 19 (five injections per week). The dose of 100mg/kg cambinol is the highest dose that could be administered as a single i.v. injection due to limited solubility of the drug. Tumor size is measured thrice a week using caliper and the tumor volumes are calculated. |
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 )
