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Cambinol  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（50 mg/mL 超声）
产品描述：基本信息 产品编号：C10816 产品名称：Cambinol CAS: 14513-15-6   储存条件 粉末 -20℃（避光） 四年 分子式： C21H16N2O2S 溶于液体 -80℃ 两年 分子量 360.43 -20℃ 一个月 化学名：  5-((2-hydroxynaphthalen-1-yl)methyl)-6-phenyl-2-thioxo-2,3-dihydropyrimidin-4(1H)-one   Solubility (25°C)   体外 DMSO 21mg/mL (58.26mM) Ethanol Insoluble Water Insoluble 体内 现配现用   ＜1mg/ml表示微溶或不溶。 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。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7745mL 13.8723mL 27.7446mL 5mM 0.5549mL 2.7745mL 5.5489mL 10mM 0.2774mL 1.3872mL 2.7745mL 50mM 0.0555mL 0.2774mL 0.5549mL   生物活性 产品描述 一种 SIRT1 和 SIRT2 的抑制剂，IC50 值分别为 56μM 和 59μM。 靶点/IC50 SIRT1 56μM (IC50) SIRT2 59μM (IC50)   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.   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 .   推荐实验方法(仅供参考) 细胞实验： 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. 动物实验:   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.
保存条件：-20℃ 避光

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