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尾孢素酰胺  ≥98%

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包装规格：500ug 1mg in glass bottle
产品描述：基本信息 产品编号：C10750 产品名称：Cercosporamide CAS: 131436-22-1   储存条件 粉末 -20℃ 四年 分子式： C16H13NO7 溶于液体 -80℃ 六个月 分子量 331.28 -20℃ 一个月 化学名：  (9aS)-8-acetyl-1,3,7-trihydroxy-9a-methyl-9-oxodibenzofuran-4-carboxamide   Solubility (25°C)   体外 DMSO   Ethanol   Water   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。     生物活性 产品描述 一种高效的 ATP 竞争性 Pkc1 激酶抑制剂，IC50<50nM，Ki<7nM。是一种独特的 Mnk 抑制剂。 靶点/IC50 Pkc1 50nM (IC50) Pkc2 7nM (Ki) Mnk   体外研究 Cercosporamide is a broad-spectrum natural antifungal compound, is actually a selective and highly potent fungal Pkc1 kinase inhibitor. Cercosporamide, an antifungal agent that is recently shown to act as a unique Mnk inhibitor, exhibits antileukemic properties. Cercosporamide is a potent inhibitor of phosphorylation of eIF4E at Ser209 in AML cells and results in potent inhibitory effects on primitive leukemic progenitors (CFU-L) from AML patients. To determine whether Cercosporamide exhibits negative regulatory effects on cell proliferation and viability of leukemia cells, MTT assays are conducted. When U937 cells are incubated in the presence or absence of the increasing doses of Cercosporamide, a dosedependent suppression of cell growth is found. Similar experiments with comparable results are seen when the effects of Cercosporamide on MM6 and K562 cells are examined.   体内研究 Treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (P<0.011 for 10mg/kg twice-daily Cercosporamide; P<0.006 for Cercosporamide 20mg/kg daily; P<0.0374 for Ara-C). The combination of Cercosporamide 10 mg/kg twice daily plus Ara-C is significantly more effective than either agent alone (P<0.0009 vs Cercosporamide; P=0.005 vs Ara-C; P<0.0001 vs either vehicle). Cercosporamide (20mg/kg once daily) in combination with Ara-C shows similar effects, with significant inhibition of tumor growth vs captisol (P<0.0001) or water (P=0.0003), but does not show statistical significance vs Cercosporamide alone (20mg/kg) or Ara-C alone.       推荐实验方法(仅供参考) 细胞实验:   Cell Assay U937, MM6, and K562 cells are incubated for 5 days in the presence or absence of the indicated doses of Cercosporamide (1,10, and 20μM) . Cell proliferation is assessed by an MTT assay.     动物实验:   Animal Administration Mice MV4-11 cells are implanted at a density of 5×106 cells per mouse. Tumors are measured by caliper and tumor volume is calculated. Once tumors reach a group mean of 100mm3, animals are randomized to the following treatment groups: Ara-C (20mg/kg daily dosed intraperitoneally), Cercosporamide (10mg/kg twice daily, 20mg/kg daily dosed orally by gavage), Ara-C plus Cercosporamide combinations (as above), or the relative vehicle controls (captisol for Cercosporamide and water for Ara-C).
保存条件：-20℃

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