| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
2′,3′,5′-Triacetyl-5-azacytidine targets DNA methyltransferase (DNMT) through its conversion to 5-azacytidine. 5-Azacytidine is a DNA methyltransferase inhibitor that incorporates into DNA and traps DNMT enzymes, leading to DNA demethylation and reactivation of silenced genes. This mechanism makes it a valuable tool for studying epigenetic regulation and for developing epigenetic therapies.
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| ln Vitro |
In vitro, 2′,3′,5′-Triacetyl-5-azacytidine decreases promoter methylation of P15 in L1210 mouse leukemia cells at concentrations of 1 and 100 µM. Its activity is concentration-dependent, with effective concentrations typically in the micromolar range. Its ability to inhibit DNA methylation makes it a valuable tool for studying epigenetics and for developing anticancer therapeutics.
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| ln Vivo |
In vivo, 2′,3′,5′-Triacetyl-5-azacytidine is an orally bioactive prodrug of 5-azacytidine. It may be rapidly absorbed orally without formation of major metabolites in the gastrointestinal tract. Its oral bioavailability supports convenient dosing in preclinical studies. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources.
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| Enzyme Assay |
The in vitro DNA methyltransferase inhibition assay for 2′,3′,5′-Triacetyl-5-azacytidine typically uses purified DNMT enzyme or cell lysates. The assay is performed with a DNA substrate and varying concentrations of the test compound (typically 0.1 to 100 µM). DNA methylation is measured by incorporation of radiolabeled methyl groups or by bisulfite sequencing.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines (e.g., L1210 leukemia cells) are treated with 2′,3′,5′-Triacetyl-5-azacytidine at concentrations ranging from 0.1 to 100 µM for 24-72 hours. DNA methylation is assessed by bisulfite sequencing or methylation-specific PCR. Gene expression is assessed by qRT-PCR. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, animal models of cancer are used. 2′,3′,5′-Triacetyl-5-azacytidine is administered orally at doses ranging from 1 to 50 mg/kg. Tumor growth is monitored, and DNA methylation is assessed in tumor tissues. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 2′,3′,5′-Triacetyl-5-azacytidine have been partially characterized. The compound has a molecular weight of 370.31. It may be rapidly absorbed orally without formation of major metabolites in the gastrointestinal tract.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of 2′,3′,5′-Triacetyl-5-azacytidine are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg.
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| References | |
| Additional Infomation |
2′,3′,5′-Triacetyl-5-azacytidine is an orally bioactive prodrug form of 5-azacytidine, a DNA methyltransferase inhibitor. It has a molecular formula of C14H18N4O8 and a molecular weight of 370.31. It decreases promoter methylation of P15 in L1210 mouse leukemia cells. It is not approved for human use and is intended for research purposes only.
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| Molecular Formula |
C14H18N4O8
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|---|---|
| Molecular Weight |
370.3147
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| Exact Mass |
370.112
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| CAS # |
10302-78-0
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| PubChem CID |
324936
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
497.3±55.0 °C at 760 mmHg
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| Flash Point |
254.6±31.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.634
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| LogP |
-0.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
676
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C([H])(C([H])(C([H])(C1([H])C([H])([H])OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)OC(C([H])([H])[H])=O)N1C([H])=NC(N([H])[H])=NC1=O
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| InChi Key |
OTQJVHISAFFLMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H18N4O8/c1-6(19)23-4-9-10(24-7(2)20)11(25-8(3)21)12(26-9)18-5-16-13(15)17-14(18)22/h5,9-12H,4H2,1-3H3,(H2,15,17,22)
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| Chemical Name |
[3,4-diacetyloxy-5-(4-amino-2-oxo-1,3,5-triazin-1-yl)oxolan-2-yl]methyl acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
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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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7004 mL | 13.5022 mL | 27.0044 mL | |
| 5 mM | 0.5401 mL | 2.7004 mL | 5.4009 mL | |
| 10 mM | 0.2700 mL | 1.3502 mL | 2.7004 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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