Date published: 2026-7-23

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Idarubicinol (CAS 86189-66-4)

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Alternate Names:
(7S,9S)-7-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-9-[(1R*)-1-hydroxyethyl]-5,12-Naphthacenedione
Application:
Idarubicinol is a 13-OH metabolite of idarubicin with cytotoxic effects on leukemia cells
CAS Number:
86189-66-4
Molecular Weight:
499.51
Molecular Formula:
C26H29NO9
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Idarubicinol is a 13-dihydro (13-OH) metabolite of idarubicin (sc-204774) which may play an important role in the clinical efficacy of idarubicin in patients with acute leukemia. Idarubicinol persists in the blood for prolonged periods after the administration of idarubicin, and is strongly cytotoxic against HL60 cells (human leukemia cells). Reduction of idarubicin in vivo is dependent upon ketone reductases, and proceeds more stereoselectively than that of most ketones giving rise to the (13S)-epimer almost exclusively. The effects of idarubicin and its metabolite idarubicinol on multicellular spheroids, a model which mimics the microregions of solid tumors has also been investigated on MCF-7 breast cancer cells. Idarubicin and idarubicinol have significant cytotoxic activity against multicellular spheroids.


Idarubicinol (CAS 86189-66-4) References

  1. Determination of idarubicin and idarubicinol in rat plasma using reversed-phase high-performance liquid chromatography and fluorescence detection.  |  Kuhlmann, O., et al. 1999. J Chromatogr B Biomed Sci Appl. 728: 279-82. PMID: 10406213
  2. Modeling the metabolism of idarubicin to idarubicinol in rat heart: effect of rutin and phenobarbital.  |  Kang, W. and Weiss, M. 2003. Drug Metab Dispos. 31: 462-8. PMID: 12642473
  3. Idarubicin and idarubicinol effects on breast cancer multicellular spheroids.  |  Orlandi, P., et al. 2005. J Chemother. 17: 663-7. PMID: 16433198
  4. Stereoselectivity of idarubicin reduction in various animal species and humans.  |  Strolin Benedetti, M., et al. 1991. Xenobiotica. 21: 473-80. PMID: 1897247
  5. In vitro evaluation of the reductive carbonyl idarubicin metabolism to evaluate inhibitors of the formation of cardiotoxic idarubicinol via carbonyl and aldo-keto reductases.  |  Bajraktari-Sylejmani, G., et al. 2024. Arch Toxicol. 98: 807-820. PMID: 38175295
  6. Influence of idarubicinol on the antileukemic effect of idarubicin.  |  Fukushima, T., et al. 1994. Leuk Res. 18: 943-7. PMID: 7996875
  7. Cellular pharmacology of idarubicinol in multidrug-resistant LoVo cell lines.  |  Toffoli, G., et al. 1996. Int J Cancer. 67: 129-37. PMID: 8690513
  8. Comparative activity of idarubicin and idarubicinol in combination with cyclosporin A in multidrug-resistant leukemia cells.  |  Tolomeo, M., et al. 1996. Cancer Chemother Pharmacol. 39: 157-61. PMID: 8995514
  9. Determination of idarubicin and idarubicinol in plasma by capillary electrophoresis.  |  Hempel, G., et al. 1997. J Chromatogr B Biomed Sci Appl. 698: 287-92. PMID: 9367219
  10. Effect of PSC 833 on the cytotoxicity of idarubicin and idarubicinol in multidrug-resistant K562 cells.  |  Fukushima, T., et al. 1999. Leuk Res. 23: 37-42. PMID: 9933133

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Idarubicinol, 500 µg

sc-488055
500 µg
$430.00