Cercosporamide
(Synonyms: 尾孢素酰胺,(-)-Cercosporamide) 目录号 : GC15391
A potent inhibitor of fungal Pkc1 and mammalian Mnk isoforms
Cas No.:131436-22-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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[2]. |
Animal experiment: | Mice[2]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 100 mm3, animals are randomized to the following treatment groups: Ara-C (20 mg/kg daily dosed intraperitoneally), Cercosporamide (10 mg/kg twice daily, 20 mg/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)[2]. |
References: [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. | |
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of
Cercosporamide is a broad-spectrum natural antifungal compound, is actually a selective and highly potent fungal Pkc1 kinase inhibitor[1]. 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[2].
Treatment with Cercosporamide or Ara-C alone significantly suppresses xenograft growth when compared with the respective vehicle (P
References:
[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.
| Cas No. | 131436-22-1 | SDF | |
| 别名 | 尾孢素酰胺,(-)-Cercosporamide | ||
| 化学名 | (9aS)-8-acetyl-1,3,7-trihydroxy-9a-methyl-9-oxodibenzofuran-4-carboxamide | ||
| Canonical SMILES | CC(=O)C1=C(C=C2C(C1=O)(C3=C(C=C(C(=C3O2)C(=O)N)O)O)C)O | ||
| 分子式 | C16H13NO7 | 分子量 | 331.28 |
| 溶解度 | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0186 mL | 15.093 mL | 30.1859 mL |
| 5 mM | 0.6037 mL | 3.0186 mL | 6.0372 mL |
| 10 mM | 0.3019 mL | 1.5093 mL | 3.0186 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。