product name Azacitidine
Description: 5-Azacytidine (also known as 5-AzaC), a compound belonging to a class of cytosine analogues, is a DNA methyl transferase (DNMT) inhibitor that exerts potent cytotoxicity against multiple myeloma (MM) cells, including MM.1S, MM.1R, RPMI-8266, RPMI-LR5, RPMI-Dox40 and Patient-derived MM, with the half maximal inhibition concentration IC50 values of 1.5 μmol/L, 0.7 μmol/L, 1.1 μmol/L, 2.5 μmol/L, 3.2 μmol/L and 1.5 μmol/L respectively.
References: Oncogene. 2002 Aug 12;21(35):5483-95; J Biol Chem. 1982 Feb 25;257(4):2041-8.
244.2
Formula
C8H12N4O5
CAS No.
320-67-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (196.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
NSC 102816
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410657
| In Vitro |
In vitro activity: Azacitidine is widely used to demonstrate the correlation between loss of methylation in specifc gene regions and activation of the associated genes. After incorporation into DNA, Azacitidine inhibits DNA methyltransferase noncompetitively, causing a block in cytosine methylation in newly replicated DNA but not in resting, nondividing cells. Azacitidine induces differentiation of Friend Erythroleukemia Cell C3H10T1/2 with myotube formation. Azacitidine can be activated to the nucleoside triphosphate and incorporate into both DNA and RNA, leading to inhibition of DNA, RNA and protein synthesis in normal eukaryotic cells and in cancer cell lines, which could finally leads to cell death. Azacitidine also inhibits the incorporation of purine metabolites into macromolecules. Azacitidine inhibits the L1210 cells growth with IC50 and of 0.019 μg/mL. Kinase Assay: Cell Assay: 5 mL of L1210 cells (5 × 103 cells/mL) are incubated with Azacitidine at 37 ℃ for 3 days. Cell number is determined twice a day for 3 days by means of a Model A Coulter counter. |
|---|---|
| In Vivo | Azacitidine inhibits polynucleotide synthesis in leukemic BDF1 mice. Azacitidine (3 mg/kg, i.p.) increases the mean survival time in leukemic BDF1 mice inoculated with Ll210 ascites tumor cells. Azacitidine markedly suppresses all enzymes activity in the polyamine-biosynthetic pathway, including ornithine decarboxylase activity. putrescine-dependent S-adenosyl-L-methionine decarboxylase activity, and spermidine-dependent S-adenosyl-L-methionine decarboxylase activity. Azacitidine also inhibits the accumulations of polyamines in leukemic mice. |
| Animal model | BDF1 mice bearing lymphoid leukemia L1210 |
| Formulation & Dosage | Dissolved in 0.85% NaCl solution; 3 mg/kg; i.p. injection |
| References | Oncogene. 2002 Aug 12;21(35):5483-95; J Biol Chem. 1982 Feb 25;257(4):2041-8. |
