Idarubicin hydrochloride

An anthracycline antileukemic that inserts into DNA and prevents DNA unwinding by interfering with the enzyme Topoisomerase II in cancer cells; inhibits the proliferation of MCF-7 cells with IC50 of 0.1 uM; also induces histone eviction from chromatin.Chemotherapeutic Agents Approved (In Vitro) :The IC50 of idarubicin is 3.3±0.4 ng/mL on MCF-7 monolayers and 7.9±1.1 ng/mL in multicellular spheroids. Idarubicin has shown a greater cytotoxicity than daunorubicin or doxorubicin in various in vitro systems. This has been attributed to a better ability of idarubicin to induce the formation of topoisomerase II -mediated DNA breaks.Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively. Idarubicin produces a concentration-dependent reduction in cell growth, with an IC50 value of approximately 0.01 μM. Idarubicin produced a concentration-dependent inhibition of DNA synthesis.