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5-Azacytidine
- Min. Order1kg
- Purity99%
- Cas No320-67-2
- Supply Ability100kg
- Update time2025-10-13
| Product Name | 5-Azacytidine |
| CAS No | 320-67-2 |
| EC-No | |
| Min. Order | 1kg |
| Purity | 99% |
| Supply Ability | 100kg |
| Release date | 2025/10/13 |
PRODUCT INFORMATION
Names
| Name | 5-azacytidine |
|---|---|
| Synonym | More Synonyms |
Azacitidine (5-Azacytidine) Biological Activity
| Description | 5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. |
|---|---|
| Related Catalog | Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Epigenetics >> DNA Methyltransferase Signaling Pathways >> Cell Cycle/DNA Damage >> Nucleoside Antimetabolite/Analog Research Areas >> Cancer |
| Target | DNMT1 Nucleoside Antimetabolite/Analog Autophagy |
| In Vitro | Unmethylated CpG islands associated with a variety of genes become partially or fully methylated in tumors and can be reactivated by 5-Azacytidine[1]. 5-Azacytidine acts as weak inducers of erythroid differentiation of Friend erythroleukemia cells in the same concentration range where they affect DNA methyltransferase activity[2]. 5-Azacytidine inhibits L1210 cells with ID50 and ID90 values of 0.019 and circa 0.15 μg/mL, respectively[3]. |
| In Vivo | TdR-3H incorporation is significantly inhibited when the animals are exposed to 5-Azacitidine (100 mg/kg, i.p.) for 2 hr or longer[3]. |
| Kinase Assay | A crude cell-free extract is isolated from LI 210 cells in culture by suspension of the cells in a given volume of 0.05mol/LTris-HCl buffer, pH 7.4, and sonic extraction with a Biosonik at 70% maximal output for 30 sec. The supernatant is collected after centrifugation at 105,000 × g for 60 min (4°C) in a Model L Spinco ultracentrifuge. The final protein concentration of the cell-free extracts is approximately 3 mg/mL. The extracts are used as the source of enzymes. Ribonucleotide reductase activity is measured. A unit of enzyme is defined as the amount that catalyzed dCMP synthesis at a rate of 1 mμmole/hr. The assay systems for the measurement of pyrimidine nucleoside (CR) and deoxynucleoside (TdR, CdR) kinases are essentially those described by Chu and Fischer. However, reactions are terminated by heating for 2 min in a boiling water bath, and the phosphorylated derivatives are isolated according to the method of Bach. Fifty-jul aliquots are applied to 1-inch discs of diethylaminoethyl paper, which are then placed in counting vials and eluted with 0.5 mL of 0.5 mol/LPCA. After 1 hr, 12 mL of Diotol are added, and the radioactivity is determined. |
| Cell Assay | Twenty mL of cells (circa 1×104 cells/mL) are pipetted into sterilized culture tubes with screw caps and incubated at 37°C overnight. The experiment is initiated by the addition of 1 mL of 5-Azacytidine (5-azaCR) or medium for a given period (from 0 to 240 min) prior to the addition of 1 mL of metabolite (or medium). Cell growth is determined twice a day for 3 days by means of a Model A Coulter counter. To determine IDSO and ID90 values, 5 mL of L1210 cells (5×103 cells/mL) are incubated with the drug at 37°C for 3 days, and cell growth is determined. |
| Animal Admin | For the in vivo experiments, leukemic mice (bearing circa 1×103 cells/animal) are given injections i.p. with 0.2 mL of 5-Azacytidine (5-azaCR) of a given concentration. Two hr later, the reaction is started by injecting 0.5 mL of labeled metabolite (TdR-3H or UR-3H, 10 /μCi/12.5 μg). After 1 hr, animals (3 mice/group) are killed by cervical fracture, and the ascites are treated with heparin, collected, pooled, and then centrifuged immediately in a Sorvall refrigerated centrifuge Model R2C-B at 800×g for 10 min (4°C). |
| References | [1]. Christman JK. 5-Azacytidine and 5-aza-2'-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy. Oncogene. 2002 Aug 12;21(35):5483-95. [2]. Creusot F, et al. Inhibition of DNA methyltransferase and induction of Friend erythroleukemia cell differentiation by 5-azacytidineand 5-aza-2'-deoxycytidine. J Biol Chem. 1982 Feb 25;257(4):2041-8. [3]. Li LH,et al. Cytotoxicity and mode of action of 5-azacytidine on L1210 leukemia. Cancer Res. 1970 Nov;30(11):2760-9. |
Chemical & Physical Properties
| Density | 2.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 534.5±60.0 °C at 760 mmHg |
| Melting Point | 226-232 °C (dec.)(lit.) |
| Molecular Formula | C8H12N4O5 |
| Molecular Weight | 244.205 |
| Flash Point | 277.0±32.9 °C |
| Exact Mass | 244.080765 |
| PSA | 143.72000 |
| LogP | -1.99 |
| Vapour Pressure | 0.0±3.2 mmHg at 25°C |
| Index of Refraction | 1.823 |
| Water Solubility | 0.5-1.0 g/100 mL at 21 ºC |
MSDS
Azacitidine (5-Azacytidine) MSDS(Chinese) |
Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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Safety Information
| Symbol | ![]() GHS07, GHS08 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H302-H350 |
| Precautionary Statements | P201-P308 + P313 |
| Personal Protective Equipment | Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges |
| Hazard Codes | T:Toxic |
| Risk Phrases | R45;R46;R22 |
| Safety Phrases | S53-S22-S36/37/39-S45 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
| RTECS | XZ3017500 |
| HS Code | 2934999090 |
Synthetic Route
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| Literature: ScinoPharm Taiwan Ltd. Patent: US2010/36112 A1, 2010 ; Location in patent: Page/Page column 7 ; |
![]() Beta-D-Ribofura... CAS#:13035-61-5 ~40% ![]() Azacitidine (5-... CAS#:320-67-2 |
| Literature: Ionescu, Dumitru; Blumbergs, Peter Patent: US2004/186283 A1, 2004 ; Location in patent: Page 8 ; |
![]() 2',3',5'-triace... CAS#:10302-78-0 ~75% ![]() Azacitidine (5-... CAS#:320-67-2 |
| Literature: SICOR INC.; BIGATTI, Ettore; LUX, Giovanna; PAIOCCHI, Maurizio; GIOLITO, Andrea; TOSI, Simone Patent: WO2010/17374 A1, 2010 ; Location in patent: Page/Page column 18 ; |
Precursor & DownStream
| Precursor 9 | Previous 1/3 Next |
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| DownStream 1 | |
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Customs
| HS Code | 2934999090 |
|---|---|
| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Company Profile
Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions.
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Company Profile Introduction
Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions. With our agile custom synthesis capabilities and responsive supply chain system, our products have gained widespread adoption across Asian markets including Japan, South Korea, Singapore, and Malaysia, while also expanding deeply into Europe and the Americas. We have forged long-term strategic partnerships with numerous leading global enterprises in the sector. "Driving value through technology and earning trust through service" is our core mission. Looking ahead, we will continue to focus on technological breakthroughs and green innovation in new materials, collaborating with partners to build a high-quality industrial ecosystem and provide globally competitive solutions with greater foresight.
China


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CAS#:65370-90-3

