Idarubicin Hydrochloride is the hydrochloride salt of Idarubicin, an anthracycline antibiotic and daunomycin analog with antimicrobial and anti-cancer antileukemic properties. It is a Topoisomerase II inhibitor, interfering with DNA replication and RNA transcription. The compound was developed by Johnson & Johnson. Idarubicin is metabolished into Idarubicinol (a 13-dihydro derivative) which is more stable than the parent form and just as active in in vitro models. The product is used in apoptosis research. Idarubicin Hydrochloride is soluble in DMSO.
| Mechanism of Action | Idarubicin has a higher DNA binding capacity and greater cytotoxicity than daunorubicin. It is a Topoisomerase II inhibitor, specifically the subunits GyrA and GyrB. It acts by stabilizing enzyme-DNA complexes wherein DNA strands are cut and covalently linked to the protein. The antineoplastic mechanism is mainly attributed to its DNA intercalating ability and its inhibition of Topo II impairs cellular DNA replication. |
| Spectrum | Idarubicin has activity against bacteria including Gram-positive cocci (MRSA, S. epidermidis) and yeasts. |
| Cancer Applications | The effect of Idarubicin and idarubicinol on multicellular spheroids, a model that mimics the microregions of solid tumors, to examine in vitro cytotoxicity on MCF-7 breast cancer cells. Authors found Idarubicin and Idrubicinol have significant cytotoxic activity against multicellular spheroids with an IC50 of 7.9 ng/ml (Orlandi et al, 2005). |
| Molecular Formula |
C26H27NO9 · HCl |
| References |
Kinnunen U, Syrjälä H, Koistinen P, Koskela M (2009) Idarubicin inhibits the growth of bacteria and yeasts in an automated blood culture system. Eur J Clin Microbiol Infect Dis. 28(3):301-303. PMID 18763001 López-Lázaro M et al (2007) Curcumin induces high levels of topoisomerase I- and II-DNA complexes in K562 leukemia cells. J Nat Prod. 70(12):1884-1888. PMID 18076140 Robert J (1993) Clinical pharmacokinetics of idarubicin. Clin Pharmacokinet. 24(4):275-288. Erratum in: Clin Pharmacokinet 25(4):350. PMID 8491056 She, Pengfei et al. (2020) Insights into Idarubicin antimicrobial activity against methicillin-resistant Staphylococcus aureus. Virulence 11(1): 636-651 PMID 32423280
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