Biological Activity
Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription.
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[1]. 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[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 cell growth, with an IC50 value of approximately 0.01 μM. Idarubicin produced a concentration-dependent inhibition of DNA synthesis[4].
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
Cell Assay
Stock solutions of idarubicin hydrochloride is dissolved in distilled water (1 mg/mL). MCF-7 monolayer are exposed to idarubicin or its metabolite idarubicinol at 0.01, 0.1, 1, 10, 100, and 1000 ng/mL for 24 hours. Multicellular spheroids are exposed to the same range of idarubicin and idarubicinol concentration as monolayers (0.01-1000 ng/mL) for 24 h and, in separate experiments, at the drug concentration of 100 ng/mL for 6, 12, 24 and 48 h. The inhibition of cell proliferation is determined by counting the viable cells with an hemocytometer. Results are expressed as percentage of cell survival vs. control cultures[1].
References & source
[1]. Orlandi P, et al. Idarubicin and idarubicinol effects on breast cancer multicellular spheroids. J Chemother. 2005 Dec;17(6):663-7.
[2]. Robert J. Clinical pharmacokinetics of idarubicin. Clin Pharmacokinet. 1993 Apr;24(4):275-88.
[3]. Siegsmund MJ, et al. Enhanced in vitro cytotoxicity of idarubicin compared to epirubicin and doxorubicin in rat prostate carcinoma cells. Eur Urol. 1997;31(3):365-70.
[4]. Gewirtz DA, et al. Induction of DNA damage, inhibition of DNA synthesis and suppression of c-myc expression by the anthracycline analog, idarubicin (4-demethoxy-daunorubicin) in the MCF-7 breast tumor cell line. Cancer Chemother Pharmacol. 1998;41(5):361-
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
