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Decitabine (NSC127716, 5AZA-CdR).

Decitabine 是一种胞嘧啶类似物，为 DNA methyltransferase 抑制剂。

目录号: PC10024 纯度: ≥98%

CAS No. :2353-33-5

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中文名称	Decitabine (NSC127716, 5AZA-CdR).
中文别名	5-氮杂-2-脱氧胞苷;2'-脱氧-5-氮杂胞啶;地西他宾;5-氮杂-2'-脱氧胞苷酸;地西他滨(抗癌);地西他滨杂质;5-氮杂-2'-脱氧胞苷;5-氮杂-2'-脱氧胞嘧啶核苷;5-Aza-2'-deoxycytidine 5-氮杂-2'-脱氧胞嘧啶核苷;5-氮杂-2’-脱氧胞苷;5-氮杂-2''-脱氧胞苷;地西他滨;地西他滨(5-氮杂-2'-脱氧胞苷);地西他滨,5-氮杂-2'-脱氧胞嘧啶核苷;地西他滨标准品;脱氧氮杂胞苷;外-3,6-环氧-1,2,3,6-四氢苯二甲酸;5-氮杂-1-(2-脱氧-β-D-氟合亚硝脲)胞嘧啶;5-氮杂-2-脱氧胞嘧啶核苷;5-氮杂-2'-脱氧胞嘧啶核苷(标准品);地西他滨 5-氮杂-1-(2-脱氧-β-D-呋喃核糖基)胞嘧啶
英文名称	Decitabine
英文别名	5-Aza-2'-deoxycytidine;4-Amino-1-(2-deoxy-β-D-erythro-pentofuranosyl)-1,3,5-triazin-2(1H)-one;4-Amino-1-(2-deoxy-β-D-ribofuranosyl)-1,3,5-triazin-2(1H)-one;Decitabine(NSC127716);Decitabine(5-aza-2'-deoxycytidine,NSC127716);5-Aza-2'-deoxycytidine (Decitabine);5-Aza-2zzhlxy-deoxycytidine (Decitabine);4-aMino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxyMethyl)oxolan-2-yl]-1,2-dihydro-1,3,5-triazin-2-one; Decitabine;2'-deoxy-5-azacytidine;4-Amino-1-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one;5-Aza-2’-deoxy Cytidine;Decitabine (Dacogen®,NSC 127716,5-Aza-2'-deoxycytidine, 5AZA-CdR); 5-Aza-1-(2-deoxy-β-D-ribofuranosyl)cytosine;5-Aza-2‘-deoxycytidine;5-Aza-2′-deoxycytidine;5-AZA-CDR;5-AZA-DC;5-azadeoxycytidine;5-DEOXY-2'-AZACYTIDINE;Dacogen;NSC127716;2′-Deoxy-5-azacytidine;s-Triazin-2(1H)-one,4-amino-1-(2-deoxy-b-D-erythro-pentofuranosyl)-(7CI,8CI);2-Desoxy-5-azacytidine;DAC;1,3,5-Triazin-2(1H)-one,4-amino-1-(2-deoxy-b-D-erythro-pentofuranosyl)-;b-Decitabine;4-Amino-1-(2-deoxy-beta-D-erythro-pentofuranosyl)-1,3,5-triazin-2(1H)-one;Decitabine;AzadC;Dezocitidine;5-aza-2-deoxycytidine;5A2dc;MLS001332587;5-Deoxy-2′-azacytidine;5-Aza-2′-Deoxycytidine;4-Amino-1-(2-deoxy-beta-D-erythro-pentofuranosyl);4-Amino-1-(2-deoxy-beta-D-erythro-pentofuranosyl)-s-triazin-2(1H)-one;4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymet
Cas No.	2353-33-5
分子式	C₈H₁₂N₄O₄
分子量	228.21
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.

性状

Solid

IC50 & Target[1][2]

DNMT1

DNMT3A

DNMT3B

体外研究(In Vitro)

Decitabine treatment significantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours after exposure to decitabine. Decitabine induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability, and up-regulates E-cadherin expression for EBVaGC.
Only high concentrations (10 μM) Decitabine (0.1-1 μM; 24-72 hours) results in a G2 phase arrest, which is accompanied by a reduction of cells in G1 phase.
Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells.

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

Cell Cycle Analysis

Cell Line:	HCT116 cells
Concentration:	0.1, 1, 10 μM
Incubation Time:	24, 48, 72 hours
Result:	Only high drug concentrations (10 μM) resulted in a G2 phase arrest, which was accompanied by a reduction of cells in G1 phase.

体内研究(In Vivo)

Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs in female CD-1 mice, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels.
Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors established in C57BL/6 Mice.

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

Animal Model:	C57BL/6 mice (bearing EL4 cells)
Dosage:	1.0 mg/kg
Administration:	Intraperitoneal injection; once daily for 5 consecutive days
Result:	Caused continuous tumor regression even after Decitabine treatment was stopped.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Nakamura M, et al. Decitabine inhibits tumor cell proliferation and up-regulates E-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2016 Jul 19. [Information]

[2]. Parker WB. Enzymology of purine and pyrimidine antimetabolites used in the treatment of cancer. Chem Rev. 2009 Jul;109(7):2880-93. [Information]

[3]. Hagemann S, et al. Azacytidine and decitabine induce gene-specific and non-random DNA demethylation in human cancer cell lines. PLoS One. 2011 Mar 7;6(3):e17388. [Information]

[4]. Requena CE, et al. The nucleotidohydrolases DCTPP1 and dUTPase are involved in the cellular response to decitabine. Biochem J. 2016 Jun 20. [Information]

[5]. Terse P, et al. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice. Int J Toxicol. 2014 Mar-Apr;33(2):75-85. [Information]

[6]. Yu J, et al. DNA methyltransferase expression in triple-negative breast cancer predicts sensitivity to decitabine. J Clin Invest. 2018 Jun 1;128(6):2376-2388. [Information]

[7]. Wang LX, et al. Low dose decitabine treatment induces CD80 expression in cancer cells and stimulates tumorspecific cytotoxic T lymphocyte responses. PLoS One. 2013 May 9;8(5):e62924. [Information]

溶解度数据

体外研究:

DMSO : ≥ 50 mg/mL (219.10 mM)

H₂O : 20 mg/mL (87.64 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	4.3819 mL	21.9096 mL	43.8193 mL
5 mM	0.8764 mL	4.3819 mL	8.7639 mL
10 mM	0.4382 mL	2.1910 mL	4.3819 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 (protect from light)。-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: 10 mg/mL (43.82 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 (10.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.95 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 (10.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.95 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 (10.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.95 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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