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Cercosporamide

产品编号 T10764 CAS 131436-22-1

别名: (-)-Cercosporamide

Cercosporamide is a ATP-competitive Pkc1 kinase inhibitor (IC50 <50 nM; Ki <7 nM). It also is a unique Mnk inhibitor.

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Cercosporamide, CAS 131436-22-1

规格	价格/CNY		货期	数量
500 μg	￥ 4,230		35日内发货
2500 μg	￥ 19,000		35日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Cercosporamide is a ATP-competitive Pkc1 kinase inhibitor (IC50 <50 nM; Ki <7 nM). It also is a unique Mnk inhibitor.
靶点活性	MNK:50 nM, PKC1:50 nM, PKC1:7 nM (ki)
体外活性	Cercosporamide is a broad-spectrum natural antifungal compound and a selective and highly potent fungal Pkc1 kinase inhibitor [1]. Cercosporamide is recently shown to act as a unique Mnk inhibitor with 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. When U937 cells are incubated in the presence or absence of the increasing doses of Cercosporamide, 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 [2].
体内活性	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. 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 [2].

别名	(-)-Cercosporamide
分子量	331.28
分子式	C16H13NO7
CAS No.	131436-22-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Sussman A, et al. Discovery of Cercosporamide, a known antifungal natural product, as a selective Pkc1 kinase inhibitor through high-throughput screening. Eukaryot Cell. 2004 Aug;3(4):932-43. 2. Altman JK, et al. Inhibition of Mnk kinase activity by Cercosporamide and suppressive effects on acute myeloid leukemia precursors. Blood. 2013 May 2;121(18):3675-81.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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