what is 5 Azacytidine?
5 Azacitidine, chemical name 1- (β - D-ribofuranosyl) -4-amino-1,3,5-triazin-2 (1H) - one, also known as 5-azacytidine or azacytidine, is a white needle shaped crystal; It is a DNA methyltransferase inhibitor that was first launched in the United States in July 2004; It is a cell cycle specific drug that acts on the S phase, rapidly phosphorylates and infiltrates RNA (ribonucleic acid) and DNA (deoxyribonucleic acid), and inhibits protein synthesis by disrupting the smooth translation of nucleic acid into protein. It can also affect pyrimidine synthesis by inhibiting orotate nucleotide decarboxylase; Clinically, it is mainly used for the treatment of myelodysplastic syndrome, including refractory anemia, refractory anemia with increased circular iron granulocytes, accompanied by neutropenia, thrombocytopenia or requiring blood transfusion, refractory anemia with increased primitive cells, refractory anemia with increased primitive cells transformation type, and five subtypes of chronic myelomonocytic leukemia
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Product name |
5 Azacitidine |
|
CAS |
320-67-2 |
|
|
Molecular formula |
C8H12N4O5 | |
|
Molecular weight |
244.2 | |
|
EINECS Number |
206-280-2 | |
|
Storage condition |
-20°C | |
|
Appearance |
White powder | |
|
Boiling point |
387.12°C (rough estimate) | |
| Solubility | Soluble in DMSO (up to 25mg/ml) or water (up to 12mg/ml) |
What are the uses of 5 Azacytidine?

5-Azacytidine is an anti metabolic drug. The main indication is acute myeloid leukemia that is ineffective with conventional treatment. It is also used for breast cancer, melanoma, intestinal cancer, etc. The toxicity mainly manifests as leukopenia, thrombocytopenia, and anemia. Nausea and vomiting are common adverse reactions that can be improved by prolonged infusion or by using antiemetic drugs 24 to 48 hours before treatment. Other toxic effects include diarrhea, neuromuscular disorders, fever, hypotension, and rash. The preparation should be freshly prepared 3-4 hours before use.
5-Azacytidine is also a potent growth inhibitor and cytotoxic agent that inhibits DNA methyltransferase, an important regulatory mechanism for gene expression, gene activation, and silencing; Cancer adjuvant with weak antibody activity (Gram positive); Used to study the molecular effects of DNA merging during DNA methylation process
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Product Specification
|
Test Items |
Specification |
Test Result |
|
Appearance |
white crystalline powder |
Complies |
|
Identification |
HPLC should correspond to reference |
Complies |
|
IR should correspond to reference |
Complies |
|
|
Particle size d0.9 |
≤15 |
7μm |
|
water |
≤0.5% |
0.3% |
|
Heavy Metals |
≤10ppm |
<10ppm |
|
Total impurities |
≤2.0% |
0.08% |
|
Assay(on anhydrous basis) |
98~102% |
99.6% |
What are the pharmacological effects of 5 azacitidine?

5 Azacitidine exerts its anti-tumor effect by reducing DNA methylation and directly causing cytotoxicity to bone marrow abnormal hematopoietic cells. In vitro studies have shown that the concentration of this product at which DNA methylation is maximally inhibited does not significantly hinder DNA synthesis. The phenomenon of low methylation can restore normal function of genes closely related to cell differentiation and proliferation. The cytotoxic effect of this product can cause the death of rapidly proliferating cells, including cancer cells that have lost normal mechanism control, while non proliferating cells are relatively insensitive to this product.
How to prepare 5-Azacytidine?
(1) The synthesis of N-trimethylsilyl-4-trimethylsiloxy-2-amino-1,3,5-triazine (intermediate I) was carried out by adding HMDS1L, 200g of 5-azacytosine, and 20g of ammonium sulfate to a 5L four necked flask. The mixture was heated and refluxed for 24 hours to obtain a clear solution. The solution was cooled to 60 ° C and 2L of 1,2-dichloroethane was added to 80 ° C. The reaction was stirred for 8 hours, and the reaction was completed. The mixture was then cooled to 5-10 ° C for later use.

(3) The synthesis of 5 azacitidine involves transferring the viscous substance into a 3L four necked bottle with 2L of methanol, adding 30g of freshly prepared sodium methoxide, stirring at room temperature overnight, filtering, and obtaining 272g of white solid with a melting point of 228-230 ℃. 256g of white solid is obtained by recrystallization from pyridine.
How and where to buy 5-Azacytidine wholesale?
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Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
|
3-7 days |
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Suitable for under 50kg. |
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Suitable for more than 50kg. |
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15-60 days |
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