尾孢素酰胺
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- CAS号:
- 131436-22-1
- 英文名:
- Cercosporamide
- 英文别名:
- Cercosporamide;(-)-CERCOSPORAMIDE;4-Dibenzofurancarboxamide;Cercosporamide
((-)-Cercosporamide);Cercosporamide from Cercosporidium henningsii;(R)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9aβ-methyl-9-oxodibenzofuran-4-carboxamide;(9aS)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-4-dibenzofurancaboxamide;4-Dibenzofurancarboxamide, 8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (9aS)-
- 中文名:
- 尾孢素酰胺
- 中文别名:
- 尾孢素酰胺;化合物 T10764;C287456] CERCOSPORAMIDE,MNK2抑制剂
- CBNumber:
- CB11120153
- 分子式:
- C16H13NO7
- 分子量:
- 331.28
- MOL File:
- 131436-22-1.mol
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尾孢素酰胺化学性质
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沸点:
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582.5±50.0 °C(Predicted)
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密度:
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1.70±0.1 g/cm3(Predicted)
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储存条件:
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-20°C
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溶解度:
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chloroform: soluble1mg/mL
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形态:
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Powder
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酸度系数(pKa):
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11.89±0.70(Predicted)
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尾孢素酰胺性质、用途与生产工艺
Cercosporamide 是一种高效的 ATP 竞争性 Pkc1 激酶抑制剂，IC50 sub><50 nM，Ki<7 nM。Cercosporamide 是一种独特的 Mnk 抑制剂。
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Pkc1
50 nM (IC
50
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Pkc1
7 nM (Ki)
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Mnk
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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.
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.
尾孢素酰胺
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-16982 | 尾孢素酰胺
Cercosporamide | 131436-22-1 | 500μg | 9500元 |
| 2023/10/26 | HY-16982 | 尾孢素酰胺
Cercosporamide | 131436-22-1 | 1mg | 16000元 |
尾孢素酰胺
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尾孢素酰胺国内生产厂家
131436-22-1, 尾孢素酰胺 相关搜索:
- Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Inhibitors
- Heterocycles
- 微生物代谢物
- C287456] CERCOSPORAMIDE,MNK2抑制剂
- 化合物 T10764
- 尾孢素酰胺
- 131436-22-1
- 4-Dibenzofurancarboxamide, 8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (9aS)-
- Cercosporamide
((-)-Cercosporamide)
- (-)-CERCOSPORAMIDE
- (9aS)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-4-dibenzofurancaboxamide
- Cercosporamide from Cercosporidium henningsii
- 4-Dibenzofurancarboxamide
- (R)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9aβ-methyl-9-oxodibenzofuran-4-carboxamide
- Cercosporamide