Decitabine(NSC127716, 5AZA-CdR) (Synonyms: DAC, 5aza2’Deoxycytidine, NSC 127716) |
| Catalog No.GC15255 |
Decitabine(DAC) is a deoxycytidine analogue antimetabolite with oral bioactivity and functions as an inhibitor of DNA methyltransferase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2353-33-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
|
Cell lines |
SNU719, NCC24, and KATOIII cells |
|
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. |
|
Reaction Conditions |
10 µM; 0-120hs |
|
Applications |
Decitabine treatment significantly inhibited cell growth. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6 Mice |
|
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. |
|
Dosage form |
1.0 mg/kg; i.p.; 5days |
|
Applications |
Decitabine treatment inhibits tumorigenesis and leads to regression of established tumors in mice. |
|
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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| Cas No. | 2353-33-5 | SDF | |
| Synonyms | DAC, 5aza2’Deoxycytidine, NSC 127716 | ||
| Chemical Name | 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 | ||
| Formula | C8H12N4O4 | M.Wt | 228.08 |
| Solubility | ≥ 11.4 mg/mL in DMSO, ≥ 23.3 mg/mL in Water with gentle warming | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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