2016年9月19日星期一

Azacitidine


Azacitidine (INN; trade name Vidaza) is a chemical analog of cytidine, a nucleoside in DNA and RNA. Azacitidine and its deoxy derivative, decitabine (also known as 5-aza-2′deoxycytidine), are used in the treatment of myelodysplastic syndrome. Both drugs were first synthesized in Czechoslovakia as potential chemotherapeutic agents for cancer.
Uses

Clinical

Azacitidine, marketed as Vidaza, is used mainly in the treatment of myelodysplastic syndrome, for which it received approval by the U.S. Food and Drug Administration on May 19, 2004.In two randomized controlled trials comparing azacitidine to supportive treatment, 16% of subjects with myelodysplastic syndrome who were randomized to receive azacitidine had a complete or partial normalization of blood cell counts and bone marrow morphology, compared to none who received supportive care, and about two-thirds of patients who required blood transfusions no longer needed them after receiving azacitidine.

It is also sometimes used for the treatment of acute myeloid leukemia,as a hypomethylating agent.

Non-clinical

Azacitidine can be used in vitro to remove methyl groups from DNA. This may weaken the effects of gene silencing mechanisms that occur prior to methylation. Certain methylations are believed to secure DNA in a silenced state, and therefore demethylation may reduce the stability of silencing signals and confer relative gene activation.

Azacitidine induces tumor regression on isocitrate dehydrogenase-1 mutant glioma xenografts in mice.

In research, 5-azacitidine is commonly used for promoting cardiomyocyte differentiation of adult stem cells. However, it has been suggested that this drug has a compromised efficacy as a cardiac differentiation factor because it promotes the transdifferentiation of cardiac cells to skeletal myocytes.

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Product nameAzacitidine
CAS NO.320-67-2
Synonyms5-Azacitidine
CategoryPharmaceutical Raw Materials,Active Pharmaceutical Ingredients,Bulk Drugs,Fine Chemicals.
Purity99% Azacitidine
AppearanceAzacitidine powder
Shelf life2 years for Azacitidine
UsageAzacitidine is a chemical analogue of cytidine, a nucleoside present in DNA and RNA. Azacitidine and its deoxy derivative, decitabine (also known as 5-aza-2′deoxycytidine), are used in the treatment of myelodysplastic syndrome.
StorageAzacitidine should be stored in a well-closed container at low temperature, keep away from moisture, heat and light.
Specification:
ItemsRequirementsResults
DescriptionA white or almost-white crystalline powderComplies
Loss on drying≤0.50%0.41%
Melting point228-230°C229°C
Residue on ignition≤0.10%0.06%
Heavy Metals ≤10ppmComplies
Assay(HPLC) ≥98.00%99.3%

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Notice: This product is only suitable for laboratory use, or the use of animals. It can not be used directly on the human body


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