| 中文名称: | 4E1RCat | ||||
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| 英文名称: | 4E1RCat | ||||
| 别名: | 4-[2,3-二氢-3-[[5-(4-硝基苯基)-2-呋喃基]亚甲基]-2-氧代-5-苯基-1H-吡咯-1-基]苯甲酸;4E1RCat 抑制剂 (Z)-4-(3-((5-(4-nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acid | ||||
| CAS No: | 328998-25-0 | 分子式: | C28H18N2O6 | 分子量: | 478.45 |
| CAS No: | 328998-25-0 | ||||
| 分子式: | C28H18N2O6 | ||||
| 分子量: | 478.45 | ||||
基本信息
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产品编号： |
E10370 |
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产品名称： |
4E1RCat |
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CAS: |
328998-25-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
478.45 |
-20℃ |
一个月 |
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化学名： |
4-[(3E)-3-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenylpyrrol-1-yl]benzoic acid |
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Solubility (25°C)： |
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体外:
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DMSO |
96 mg/mL (200.64 mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1 mM |
2.0901 mL |
10.4504 mL |
20.9008 mL |
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5 mM |
0.4180 mL |
2.0901 mL |
4.1802 mL |
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10 mM |
0.2090 mL |
1.0450 mL |
2.0901 mL |
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50 mM |
0.0418 mL |
0.2090 mL |
0.4180 mL |
生物活性
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产品描述 |
一种 cap 依赖性翻译抑制剂，能够抑制 eIF4E:eIF4GI 相互作用，IC50 值约为 4μM。 |
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靶点 |
IC50:Q4μM (eIF4E/eIF4G) |
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体外研究 |
4E1RCat is an inhibitor of eIF4E:eIF4GI interaction, with an IC50 an of -4μM. 4E1RCat binding to eIF4E also interferes with eIF4G and 4E-BP binding. 4E1RCat inhibits ribosome recruitment to mRNA in a cap-dependent manner. 4E1RCat blocks the capped mRNA translation, and the translation is activated by CDK1/CYCB1. Nearly all new protein synthesis in both mitosis and interphase is cap-dependent and -sensitive to 4E1RCat treatment, in HeLa and U2OS cells |
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体内研究 |
4E1RCat (15mg/kg, i.p.) affacts chemosensitivity of Pten+/-Eμ-Myc tumors in mice. 4E1RCat (15 mg/kg, i.p.) sensitizes Pten+/- Eμ-Myc and Tsc2+/-Eμ-Myc lymphomas to the cytotoxic effects of doxorubicin (Dxr), and 4E1RCat targets translation in mice |
推荐实验方法(仅供参考)
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Cell Assay |
TSC2+/-Eμ-Myc and Eμ-Myc lymphomas are seeded in 96-well plates at 106 cells/mL in the presence of increasing concentrations of doxorubicin (Dxr) (ranging from 3.9nM to 250nM) and 4E1RCat (ranging from 78.13nM to 10 000nM) at a constant ratio of either 20:1 or 40:1. Twenty four hours later, a MTS assay is performed. To this end, Cell Proliferation Assay is added to the plates and the plates further incubated for up to 3h, followed by measuring the OD490. Values obtained are standardized against DMSO controls |
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Animal Administration |
Mice One million secondary Pten+/-Eμ-Myc, Tsc2+/-Eμ-Myc, or Eμ-Myc lymphoma cells are injected into the tail vein of 6-8 week old female C57BL/6 mice. When tumors are palpable, mice are treated with rapamycin (4 mg/kg daily for 5 d), 4E1RCat (15mg/kg daily for 5 d), or doxorubicin (once at 10mg/kg). Compounds are administered via intraperitoneal (i.p.) injection in 5.2% PEG 400/ 5.2% Tween 80. For combination studies, rapamycin or 4E1RCat are injected i.p. daily for five consecutive days, with doxorubicin being administered once on day two. Animals are palpated daily to monitor for the onset of tumors. Tumor-free survival is defined as the time between disappearance and reappearance of tumors. Data is analyzed using the log-rank test for statistical significance presented in Kaplan-Meier format |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
