Cercosporamide (Synonyms:(--Cercosporamide))
目录号 : KM16009 CAS No. : 131436-22-1

Cercosporamide 是一种高效的 ATP 竞争性 Pkc1 激酶抑制剂,IC50<50 nM,Ki<7 nM。Cercosporamide 是一种独特的 Mnk 抑制剂。

规格 价格 是否有货 数量
500μg
In-stock
1mg
In-stock
5mg 询价 In-stock
10mg 询价 In-stock

Other Forms of Rapamycin:

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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.

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 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.

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 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.

分子式
C16H13NO7
分子量
331.28
CAS号
131436-22-1
中文名称
尾孢素酰胺
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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