5-Aza-2'-deoxycytidine C??? ??, ??, ??
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Decitabine, 5-aza-2’-deoxycytidine, has been launched for the treatment of
myelodysplastic syndromes (MDS). MDS are a set of hematologic disorders
affecting the bone marrow that result in ineffective formation and development
of blood cells. Furthermore, patients with MDS have a high risk of progressing to
acute myeloid leukemia (AML). Traditional treatments include blood transfusions,
hematopoietic growth factors, and prophylactic antibiotics, but these
measures merely improve the quality of life with questionable effects on disease
modification. While stem-cell transplantation is an aggressive, potentially curative
approach, the advanced age or the other complicating health issues of most
patients preclude them from considering this option. Recent advances in the
underlying etiology of MDS, however, have led to the development of a new
class of compounds known as ‘‘demethylating agents’’. Decitabine follows the
successful introduction of the first DNA methyltransferase inhibitor azacitidine.
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white crystalline powder
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Used as cancer treatment, in particular to inhibit the growth of pancreatic endocrine tumor cell lines.
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Fine white crystalline powder. Used as a drug.
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Probably light and air sensitive. Water soluble. Decomposes in aqueous solution at a rate that depends on pH: at pH 7 the drug is more stable than at pH 9, but is less stable than at pH 6. At pH 7 and 99°F, approximately 7% conversion occurs in 1 hour .
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5-Aza-2'-deoxycytidine is an aminoalcohol. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.
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Flash point data for 5-Aza-2'-deoxycytidine are not available. 5-Aza-2'-deoxycytidine is probably combustible.
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Cytosine analog that once incorporated into DNA acts as a suicide substrate for DNA methyltransferase. Inhibits DNA methyltransferase and results in DNA hypomethylation and activation of silent genes. Chemotherapeutic agent; suppresses growth of human tumor cell lines. Demethylates differentiation-related genes; reverses embryonic stem cell differentiation.
Safety Profile
Poison by intravenous route.Human mutation data reported. When heated todecomposition it emits toxic fumes of NOx.
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