Zebularine
(Synonyms: 2-嘧啶酮-B-核甙,NSC 309132) 目录号 : GC12153
A DNA methyltransferase inhibitor
Cas No.:3690-10-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
10T1/2 cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
30 μM; 24 hrs |
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Applications |
In 10T1/2 cells, Zebularine induced muscle cell formation. However, the 10T1/2 cells treated with Zebularine showed less muscle cell formation than those treated with either 5-Aza-CdR or 5-Aza-CR. |
| Animal experiment [1]: | |
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Animal models |
BALB/c nu/nu mice bearing EJ6 bladder cell xenografts |
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Dosage form |
500 or 1000 mg/kg; i.p. or p.o. |
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Applications |
In BALB/c nu/nu mice bearing EJ6 bladder cell xenografts, Zebularine (1000 mg/kg) significantly reduced tumor volumes when administered by intraperitoneal injection or by oral gavage. Moreover, Zebularine only showed slight cytotoxicity to tumor-bearing mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Cheng JC, Matsen CB, Gonzales FA, Ye W, Greer S, Marquez VE, Jones PA, Selker EU. Inhibition of DNA methylation and reactivation of silenced genes by zebularine. J Natl Cancer Inst. 2003 Mar 5;95(5):399-409. |
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Zebularine, a chemically stable cytidine analog containing a 2-(1H)-pyridimidinone ring, is an effective DNA methylation inhibitor which can act with DNA methyltransferases to form a covalent complex. It has been shown to cause demethylation and reactivation of a silenced and hypermethylated p16 gene. Zebularine is able to induce the myogenic phenotype in 10T1/2 cells, which is a phenomenon unique to DNA methylation inhibitors. zebularine can act as a pro-drug leading to inhibition of DNA methylation and gene activation in fungal and mammalian cells. It was the only slightly cytotoxic to T24 cells in vitro. Zebularine is stable in aqueous solution up to a pH of 12.
Reference
[1].C.B. Yoo, J.C. Cheng and P.A. Jones. Zebularine: a new drug for epigenetic therapy. Biochemical Society Transactions. 2004; 32(6): 910 – 912.
[2].Jonathan C. Cheng, Cindy B. Matsen, Felicidad A. Gonzales, Wei Ye, Sheldon Greer, Victor E. Marquez, Peter A. Jones, Eric U. Selker. Inhibition of DNA Methylation and Reactivation of Silenced Genes by Zebularine. Journal of the National Cancer Institute. 2003; 95(5): 399 – 409.
| Cas No. | 3690-10-6 | SDF | |
| 别名 | 2-嘧啶酮-B-核甙,NSC 309132 | ||
| 化学名 | 1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one | ||
| Canonical SMILES | C1=CN(C(=O)N=C1)C2C(C(C(O2)CO)O)O | ||
| 分子式 | C9H12N2O5 | 分子量 | 228.2 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 14 mg/ml,Ethanol: 0.25 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at 2-8°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 | 4.3821 mL | 21.9106 mL | 43.8212 mL |
| 5 mM | 0.8764 mL | 4.3821 mL | 8.7642 mL |
| 10 mM | 0.4382 mL | 2.1911 mL | 4.3821 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。