Decitabine(Synonyms: 地西他滨; 5-Aza-2′-deoxycytidine; 5-AZA-CdR; NSC 127716)

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Decitabine (Synonyms: 地西他滨; 5-Aza-2′-deoxycytidine; 5-AZA-CdR; NSC 127716)

Decitabine (5-Aza-2′-deoxycytidine) 是一种具有口服活性的脱氧胞苷类似物抗代谢物 (deoxycytidine analogue antimetabolite) 和 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂。Decitabine 代替 DNA 掺入胞嘧啶可以将 DNA 甲基转移酶共价捕获到 DNA 中,从而导致对该酶的不可逆抑制。Decitabine 诱导细胞 G2/M 阻滞和细胞凋亡 (apoptosis),并具有有效的抗癌活性。

Decitabine(Synonyms: 地西他滨; 5-Aza-2

Decitabine Chemical Structure

CAS No. : 2353-33-5

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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[1][2].

IC50 & Target[5]

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[1].
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[3].
Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

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[5].
Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors established in C57BL/6 Mice[7].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (bearing EL4 cells)[6]
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.

Clinical Trial

分子量

228.21

Formula

C8H12N4O4

CAS 号

2353-33-5

中文名称

地西他滨;地西他宾;2′-脱氧-5-氮杂胞啶;2′-脱氧-5-氮杂胞啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
In Vitro: 

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

*

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, 6 months; -20°C, 1 month (protect from light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: PBS

    Solubility: 10 mg/mL (43.82 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 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 ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 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.

    请依序添加每种溶剂: 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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

    [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.

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

    [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.

    [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.

    [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.

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