Mechanism of action of 1-beta-D-arabinofuranosyl-5-azacytosine and its effects in L1210 mouse leukemia cells.
Ara-5AC depresses the growth of L1210 cells in vivo in a manner that is schedule-independent and at the dose levels which are similar to those of ara-C. The 50% inhibitory concentration for ara-5AC in L1210 system is about 0.75 microM. In distinction to ara-C the drug does not elicit the proliferation of proerythroblasts in the mouse bone marrow. It is phosphorylated by dCyd kinase, and the respective Km value is 70 microM. Ara-5AC is incorporated into DNA and almost completely blocks the incorporation of thymidine at a concentration of 10 microM.
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D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001374:Azacitidine / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D001853:Bone Marrow / Q000187:drug effects; D001854:Bone Marrow Cells; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003561:Cytarabine / Q000627:therapeutic use; D000077209:Decitabine; D004353:Drug Evaluation, Preclinical; D007700:Kinetics; D007939:Leukemia L1210 / Q000378:metabolism*; D007958:Leukocyte Count; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D009705:Nucleosides / Q000378:metabolism; D010766:Phosphorylation; D013936:Thymidine / Q000378:metabolism
D000970:Antineoplastic Agents; D009705:Nucleosides; D003561:Cytarabine; C022121:fazarabine; D000077209:Decitabine; D001374:Azacitidine; D013936:Thymidine