5 Azacytidine CAS 320-67-2

5 Azacytidine CAS 320-67-2

Product Name:5 Azacytidine
CAS NO.:320-67-2
Molecular Formula:C8H12N4O5
EINECS.NO:206-280-2
Synonym:5-AZCR;5-Azacytidine;Antibiotic u 18496;Azacitidine;Azacytidine;ladakamycin;4-amino-1-beta-d-ribofuranosyl-s-triazin-2(1h)-on;mylosar;nci-c01569;nsc-102816
MOQ & Package:10g,100g,1kg etc Sub-package
Certificate:FDA,ISO,COA, HPLC, MSDS,TDS etc
Lead Time:1-3 days
Shipping:DHL,Germany DHL,Germany DPD,UPS,USPS,FedEx,EMS,By Air,By Sea etc
Store & Shelf life:Cool & dry place;36 months
Other:There are warehouses in the United States, Australia and Germany.
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Description

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

MF OF 5 Azacytidine CAS 320-67-2

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?

Symptomsofleukemia

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%

Conclusion:Conform with specification and qualified.

 

What are the pharmacological effects of 5 azacitidine?

5-Azacytidine Mechenisim on DNA cell

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.

Production of 5 Azacytidine1
(2) The synthesis of 1- (2,3,5-tri-O-acetyl - β - D-ribofuranosyl) -4-amino-1,3,5-triazin-2 (1H) one (intermediate II). To the previous reaction system, 680g of tetraacetylribose was added, and 200mL of trifluoromethanesulfonic acid trimethylsilyl ester was slowly added dropwise. The reaction was carried out at room temperature for 12 hours. The reaction solution was poured into an ice water mixture and adjusted to pH 7-8 with sodium hydroxide solution. Methyl tert butyl ether was extracted three times, 600mL each time. The organic phase was washed twice with saturated saline water, 300mL each time. The organic phases were combined and concentrated to obtain 900g of yellow viscous substance. The mass fraction measured by HPLC is 94.9%.
(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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A variety of shipping methods for you to choose

Transportation Time

Shipping method

Cargo weight requirements

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3-7 days

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UPS, USPS,FedEx, TNT,EMS

Suitable for under 50kg.
International door to door express

We have warehouses in Germany and California, USA,
and customers in Europe and America can
enjoy sending goods directly from these two places.

7-15 days

By Air

Suitable for more than 50kg.
fast and cheaper for large order

15-60 days

By Sea

Suitable for more than 500kg.
Cheapest shipping way

 

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Note: The product is for research use only and is not intended for diagnosis, treatment, disease prevention, etc.

 

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