| 规格 | 价格 | 库存 | 数量 |
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| 10 mM * 1 mL in DMSO |
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| 5mg |
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| 250mg |
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| 500mg |
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[1] US20230172936A1
| 体外研究 (In Vitro) |
接触地西他滨 96 小时后，地西他滨治疗显着降低了 SNU719、NCC24 和 KATOIII 的细胞增殖。地西他滨导致 EBVaGC 中 G2/M 期停滞和死亡，降低侵袭能力，并上调 EBVaGC 中 E-钙粘蛋白表达 [1]。只有高剂量 (10 μM) 地西他滨（0.1-1 μM；24-72 小时）才会产生 G2 期停滞，并伴有 G1 细胞减少 [3]。地西他滨上调 HeLa 细胞中的 DCTPP1 和 dUTPase 表达 [4]。
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| 体内研究 (In Vivo) |
在雌性 CD-1 小鼠中，地西他滨（1.0 mg/kg，口服）与四氢尿苷（THU）联合使用会导致严重毒性，并增加与地西他滨血浆水平相关的地西他滨毒性的易感性[5]。已建立 EL4 肿瘤的 C57BL/6 小鼠在给予地西他滨（1.0 mg/kg；腹腔注射；每天一次，持续 5 天）后显示出消退 [7]。
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| 细胞实验 |
细胞周期分析[1]
细胞类型： HCT116 细胞 测试浓度： 0.1、1、10 µM 孵育时间： 24、48、72 小时 实验结果： 只有高药物浓度 (10 µM) 才会导致 G2 期停滞，同时伴随着 G1 期细胞的减少阶段。 |
| 动物实验 |
Animal/Disease Models: C57BL/6 mice (bearing EL4 cells)[6]
Doses: 1.0 mg/kg Route of Administration: intraperitoneal (ip)injection; one time/day for 5 days consecutive Experimental Results: Caused continuous tumor regression even after Decitabine treatment was stopped. |
| 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. |
| 分子式 |
C8H12N4O4
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| 分子量 |
228.21
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| CAS号 |
2353-33-5
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| 相关CAS号 |
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| SMILES |
O=C1N([C@H]2O[C@H](CO)[C@@H](O)C2)C=NC(N)=N1
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| 化学名 |
4-amino-1-((2S,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,3,5-triazin-2(1H)-one
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| 别名 |
5-Aza-2'-deoxycytidine; deoxyazacytidine; 5-aza-dCyd; Deoxycytidine; NSC127716; NSC 127716; NSC-127716; dezocitidine; Brand name: Dacogen. Abbreviations: 5AZA; DAC
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% propylene glycol, 5% Tween 80, 65% D5W:30mg/mL Solubility in Formulation 5: 10 mg/mL (43.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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 ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02316028 | Completed | Drug: Decitabine | Liver Metastasis Colorectal Cancer |
Universitair Ziekenhuis Brussel | March 2014 | Phase 1 Phase 2 |
| NCT05960773 | Recruiting | Drug: Decitabine/cedazuridine | Mesothelioma Malignant Mesothelioma (MM) |
National Cancer Institute (NCI) | January 31, 2024 | Phase 2 |
| NCT05816356 | Recruiting | Drug: Decitabine Drug: Tetrahydrouridine |
Healthy | EpiDestiny, Inc. | March 24, 2023 | Phase 1 |
| NCT04582604 | Recruiting | Drug: modified By/Cy conditioning regimen intensified by Ruxolitinib and Decitabine |
Peripheral Blood Stem Cell Transplantation |
Chinese PLA General Hospital | September 1, 2020 | Phase 1 Phase 2 |
DNMT2-IN-1
MspI Methyltransferase (MspI )
GpC Methyltransferase (GpC )
EcoRI Methyltransferase (EcoRI Methyltransferase)
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