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产品总数：60942
| 中文名称 |
Cercosporamide
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| 中文别名 |
尾孢素酰胺;(9aS)-8-乙酰基-1,3,7-三羟基-9a-甲基-9-氧代二苯并呋喃-4-甲酰胺;二花生酸甘油酯
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| 英文名称 |
Cercosporamide
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| 英文别名 |
4-Dibenzofurancarboxamide,8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (9aS)-;Cercosporamide;(-)-Cercosporamide;(9aS)-8-acetyl-1,3,7-trihydroxy-9a-methyl-9-oxodibenzofuran-4-carboxamide;4-Dibenzofurancarboxamide;Cercosporamide from Cercosporidium henningsii;(R)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9aβ-methyl-9-oxodibenzofuran-4-carboxamide
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| Cas No. |
131436-22-1
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| 分子式 |
C16H13NO7
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| 分子量 |
331.28
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| 包装储存 |
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| 生物活性 |
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor. |
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| 性状 |
Solid |
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| IC50 & Target[1][2] |
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| 体外研究(In Vitro) |
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 dose-dependent 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. Medlife has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 体内研究(In Vivo) |
Treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (P<0.011 for 10 mg/kg twice-daily Cercosporamide; P<0.006 for Cercosporamide 20 mg/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 (20 mg/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 (20 mg/kg) or Ara-C alone. Medlife has not independently confirmed the accuracy of these methods. They are for reference only. |
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| 运输条件 |
Room temperature or refrigerated transportation. |
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| 储存方式 |
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| 结构分类 | ||||||||||
| 来源 |
Cercosporidium fungus |
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| 参考文献 |
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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