Decitabine(NSC127716, 5AZA-CdR)
(Synonyms: 地西他滨; 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716) 目录号 : GC15255
地西他滨(Decitabine, DAC)是一种具有口服生物活性的脱氧胞苷类似物抗代谢物,具有DNA甲基转移酶抑制剂的功能。
Cas No.:2353-33-5
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 |
SNU719, NCC24, and KATOIII cells |
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Preparation Method |
Cells were seeded and cultured with only RPMI-1640 supplemented with FBS for 24 hr. After 24 hr of incubation, cells were treated in the presence or absence of Decitabine for 120 hr. |
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Reaction Conditions |
10 µM; 0-120hs |
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Applications |
Decitabine treatment significantly inhibited cell growth. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 Mice |
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Preparation Method |
Decitabine was dissolved in phosphate-buffered saline (PBS) (pH 7.4) to obtain 100 µM stocks and stored at 20℃. Mice with established EL4 tumors were injected with Decitabine (1.0 mg/kg body weight in 200 µl PBS) or PBS once daily for 5 consecutive days. |
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Dosage form |
1.0 mg/kg; i.p.; 5days |
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Applications |
Decitabine treatment inhibits tumorigenesis and leads to regression of established tumors in mice. |
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References: [1]. Nakamura M, Nishikawa J,et,al. abine inhibits tumor cell proliferation and up-regulates e-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2017 Mar;89(3):508-517. doi: 10.1002/jmv.24634. Epub 2016 Nov 17. PMID: 27430892. |
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Decitabine(DAC) is a deoxycytidine analogue antimetabolite with oral bioactivity and functions as an inhibitor of DNA methyltransferase. By substituting for cytosine within DNA, Decitabine covalently captures DNA methyltransferases within the DNA structure, thereby inducing irreversible inhibition of this enzyme. Decitabine has been shown to be effective against multiple cancers, including chronic myelomonocytic leukaemia (CMML), acute myeloid leukaemia (AML) [1-3].
Decitabine (10 µM; 0-120hs) treatment significantly inhibited cell growth[4]. Decitabine-pretreated(low-dose:10 nM decitabine; 24h) CD8+ T cells have increased cytotoxicity against tumors following anti-PD-1 treatment[5]. Low-dose decitabine promoted the generation of Myeloid-derived suppressor cells (MDSCs) and enhanced their aerobic metabolism and immunosuppressive functions[6]. Decitabine treatment resulted in an increased CD4:CD8 T-cell ratio and an elevation in the central memory (Tcm, CD45RO + CD62L+) and CD25-positive populations among cultured CAR T cells when compared to CAR T cells[7].
Decitabine (1.0 mg/kg; i.p.; 5days) treatment inhibits tumorigenesis and leads to regression of established tumors in mice[8]. Decitabine (1.0 mg/kg, p.o) in combination with Tetrahydrouridine (THU) causes severe toxicity in female CD-1 mice, along with an elevated sensitivity to Decitabine toxicity correlated with Decitabine plasma levels [9].
References:
[1]. Dhillon S. Decitabine/Cedazuridine: First Approval. Drugs. 2020 Sep;80(13):1373-1378. doi: 10.1007/s40265-020-01389-7. Erratum in: Drugs. 2021 Jan;81(1):179. PMID: 32860582; PMCID: PMC7708383.
[2]. Nakamura M, Nishikawa J, et,al ecitabine inhibits tumor cell proliferation and up-regulates e-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2017 Mar;89(3):508-517. doi: 10.1002/jmv.24634. Epub 2016 Nov 17. PMID: 27430892.
[3]. Parker WB. Enzymology of purine and pyrimidine antimetabolites used in the treatment of cancer. Chem Rev. 2009 Jul;109(7):2880-93. doi: 10.1021/cr900028p. PMID: 19476376; PMCID: PMC2827868.
[4]. Nakamura M, Nishikawa J, et,al Decitabine inhibits tumor cell proliferation and up-regulates e-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2017 Mar;89(3):508-517. doi: 10.1002/jmv.24634. Epub 2016 Nov 17. PMID: 27430892.
[5]. Han P, Hou Y, et,al. Low-dose decitabine modulates T-cell homeostasis and restores immune tolerance in immune thrombocytopenia. Blood. 2021 Aug 26;138(8):674-688. doi: 10.1182/blood.2020008477. PMID: 33876188; PMCID: PMC8394906.
[6]. Ni X, Wang L, et,al. Low-dose decitabine modulates myeloid-derived suppressor cell fitness via LKB1 in immune thrombocytopenia. Blood. 2022 Dec 29;140(26):2818-2834. doi: 10.1182/blood.2022016029. PMID: 36037415.
[7]. Wang Y, Tong C, et,al. Low-dose decitabine priming endows CAR T cells with enhanced and persistent antitumour potential via epigenetic reprogramming. Nat Commun. 2021 Jan 18;12(1):409. doi: 10.1038/s41467-020-20696-x. PMID: 33462245; PMCID: PMC7814040.
[8]. Wang LX, Mei ZY, et,al. Low dose decitabine treatment induces CD80 expression in cancer cells and stimulates tumor specific cytotoxic T lymphocyte responses. PLoS One. 2013 May 9;8(5):e62924. doi: 10.1371/journal.pone.0062924. PMID: 23671644; PMCID: PMC3650049.
[9]. Terse P, Engelke K, 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. doi: 10.1177/1091581814524994. Epub 2014 Mar 17. PMID: 24639139; PMCID: PMC4001115.
地西他滨(Decitabine, DAC)是一种具有口服生物活性的脱氧胞苷类似物抗代谢物,具有DNA甲基转移酶抑制剂的功能。通过取代DNA内的胞嘧啶,Decitabine共价捕获DNA结构内的DNA甲基转移酶,从而诱导该酶的不可逆抑制。Decitabine已被证明对多种癌症有效,包括慢性髓细胞白血病(CMML)、急性髓细胞白血病(AML)[1-3]。
Decitabine (10 µM; 0-120hs) 处理显著抑制细胞生长[4]。Decitabine (low-dose:10 nM decitabine; 24h)预处理的CD8+ T细胞在抗PD-1治疗后对肿瘤的细胞毒性增加[5]。低剂量Decitabine促进髓源性抑制细胞的生成,增强其有氧代谢和免疫抑制功能[6]。与CAR - T细胞相比,Decitabine治疗导致培养的CAR - T细胞中CD4:CD8 T细胞比例升高,中枢记忆(Tcm, CD45RO + CD62L+)和CD25阳性群体升高[7]。
Decitabine治疗(1.0 mg/kg; i.p.; 5days)可抑制小鼠EL4细胞的肿瘤发生并导致已建立肿瘤的消退[8]。Decitabine(1.0 mg/kg, p.o)与四氢吡啶(THU)联用导致雌性 CD-1 小鼠发生严重毒性,并导致与 Decitabine 血浆水平相关的对 Decitabine 毒性的敏感性增加[9]。
| Cas No. | 2353-33-5 | SDF | |
| 别名 | 地西他滨; 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716 | ||
| 化学名 | 4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazin-2-one | ||
| Canonical SMILES | C1C(C(OC1N2C=NC(=NC2=O)N)CO)O | ||
| 分子式 | C8H12N4O4 | 分子量 | 228.08 |
| 溶解度 | ≥ 11.4 mg/mL in DMSO, ≥ 23.3 mg/mL in Water with gentle warming | 储存条件 | 4°C, protect from light |
| 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 | 4.3844 mL | 21.9221 mL | 43.8443 mL |
| 5 mM | 0.8769 mL | 4.3844 mL | 8.7689 mL |
| 10 mM | 0.4384 mL | 2.1922 mL | 4.3844 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。