Zebularine|3690-10-6|(NSC309132; 4-Deoxyuridine)-陌孚医药/Medlife

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Zebularine (Synonyms: NSC309132; 4-Deoxyuridine)

目录号: PC10029 纯度: ≥98%

CAS No. :3690-10-6

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PC10029-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称

Zebularine

中文别名

2-嘧啶肌苷;泽布拉林;1-(-D-呋喃核糖苷)-1,2-二氢嘧啶-2-酮;2-嘧啶酮-B-核甙;Zebularine 泽布拉林;扎布拉林

英文名称

Zebularine

英文别名

2(1H)-Pyrimidinone, 1-b-D-ribofuranosyl-;Zebularine;2-Pyrimidone-1-Beta-D-Riboside;4-Deoxyuridine;Zebularine (NSC 309132);[14C]-Zebularine;1--D-Ribofuranosyl-2(1H)-pyrimidinone;2(1H)-Pyrimidinone, 1-.β.-D-ribofuranosyl-;2(1H)-PyriMidinone,1-b-D-ribofuranosyl;4-Deoyuridine;NSC309132;Pyrimidin-2-one-D-Ribofuranoside;1-(β-D-Ribofuranosyl)-1,2-dihydropyrimidin-2-one;2-Pyrimidone-1-β-D-riboside;Pyrimidin-2-one ribonucleoside;Pyrimidin-2-one beta-ribofuranoside;Pyrimidin-2-one beta-D-ribofuranoside;1-beta-D-ribofuranosylpyrimidin-2(1H)-one;1-beta-D-ribofuranosyl-2(1H)-pyrimidinone;7A9Y5SX0GY;2(1H)-Pyrimidinone, 1-beta-D-ribofuranosyl-;1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2-dihydropyrimidin-2-one;1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)tetrahydrofura

Cas No.

3690-10-6

分子式

C₉H₁₂N₂O₅

分子量

228.20

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. Zebularine also inhibits cytidine deaminase with a K_i of 0.95 μM.

性状

Solid

IC50 & Target[1][2]

DNMT1

DNMT3a/3L

Cytidine deaminase

0.95 μM (Ki)

Autophagy

体外研究(In Vitro)

Zebularine exerts its demethylation activity by stabilizing the binding of DNMTs to DNA, hindering the methylation and decreasing the dissociation, thereby trapping the enzyme and preventing turnover even at other sites. zebularine enhances tumor cell chemo- and radiosensitivity and has antimitogenic and angiostatic activities. Zebularine inhibits DNA methylation and reactivates a gene previously silenced by methylation. Zebularine induces the myogenic phenotype in 10T1/2 cells, which is a phenomenon unique to DNA methylation inhibitors. Zebularine reactivates a silenced p16 gene and demethylated its promoter region in T24 bladder carcinoma cells. Zebularine treatment inhibits cell growth in a dose and time dependent manner with an IC₅₀ of ～100 μM and 150 μM in MDA-MB-231 and MCF-7 cells, respectively, on 96 h exposure. At high doses zebularine induced changes in apoptotic proteins in a cell line specific manner manifested by alteration in caspase-3, Bax, Bcl2 and PARP cleavage. Zebularine is also a potent competitive inhibitor of the enzyme CR deaminase. The K_i for zebularine is 0.95μM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Zebularine is only slightly cytotoxic to tumor-bearing mice. Compared with those in control mice, tumor volumes are statistically significantly reduced in mice treated with high-dose zebularine administered by intraperitoneal injection or by oral gavage. Zebularine also enhances the survival time of mice with L1210 leukemia treated with 5-AZA-CdR. About 27% of the mice treated with this drug combination has a survival time longer than the mice treated with only 5-AZA-CdR.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Champion C, et al. Mechanistic insights on the inhibition of c5 DNA methyltransferases by zebularine. PLoS One. 2010 Aug 24;5(8):e12388. [Information]

[2]. Cheng JC, et al. Inhibition of DNA methylation and reactivation of silenced genes by zebularine. J Natl Cancer Inst. 2003 Mar 5;95(5):399-409. [Information]

[3]. Billam M, et al. Effects of a novel DNA methyltransferase inhibitor zebularine on human breast cancer cells. Breast Cancer Res Treat. 2010 Apr;120(3):581-92. [Information]

[4]. Lemaire M, et al. Inhibition of cytidine deaminase by zebularine enhances the antineoplastic action of 5-aza-2-deoxycytidine. Cancer Chemother Pharmacol. 2009 Feb;63(3):411-6. [Information]

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (438.21 mM)

H₂O : 50 mg/mL (219.11 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (438.21 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.96 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.96 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.96 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.96 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.96 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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