Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits thetopoisomeraseIIinterfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibitsDNA synthesisand ofc-mycexpression. Idarubicin inhibits the growth ofbacteriaandyeasts^{[1][2][3][4][5]}.

The IC₅₀of idarubicin is 3.3 ± 0.4 ng/mL on MCF-7 monolayers and 7.9 ± 1.1 ng/mL in multicellular spheroids^[1].
Idarubicin shows a greater cytotoxicity than daunorubicin or doxorubicin in variousin vitrosystems. This has been attributed to a better ability of idarubicin to induce the formation of topoisomerase II -mediated DNA breaks^[2].
Idarubicin is about 57.5-fold and 25-fold more active than doxorubicin and epirubicin, respectively^[3].
Idarubicin produces a concentration-dependent reduction in MCF-7 cell growth, with an IC₅₀of approximately 0.01 μM. Idarubicin produces a concentration-dependent inhibition of DNA synthesis and a time- and concentration-dependent suppression of c-myc expression^[4].

497.49

C₂₆H₂₇NO₉

58957-92-9

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