Idarubicin HCl

- Overview
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    Background
    
    Idarubicin is an inhibitor of DNA topoisomerase II [1].Idarubicin is a synthetic anthracycline anticancer drug widely used in the treatment of acute myelogenous leukemia and some other hematological malignancies. It can be bioactivated by NADPH-cytochrome P450 reductase with resulting formation of single-strand breaks in DNA. This is the mechanism of Idarubicin ‘s antitumor effect [2].Idarubicin is developed in an attempt to reduce the cardiotoxicity and enhance the therapeutic efficacy of the parent compound. Unlike the parent compound, Idarubicin can be given orally and has a better therapeutic index with respect to cardiotoxicity. Idarubicin has been shown to be an effective anti-leukemic agent in children and adults [3].
    
    [1] H. Dorota Halicka, M. Fevzi Ozkaynak, Oya Levendoglu-Tugal, Claudio Sandoval , Karen Seiter, Malgorzata Kajstura, Frank Traganos, Somasunadaram Jayabose, and Zbigniew Darzynkiewicz. DNA damage response as a biomarker in treatment of leukemias. Cell Cycle. 2009, 8(11): 1720–1724.
    [2] Haydar Çelik and Emel Arinç. Evaluation of the Protective Effects of Quercetin, Rutin, Resveratrol, Naringenin and Trolox Against Idarubicin-Induced DNA Damage. J Pharm Pharmaceut Sci. 2010, 13(2): 231 – 241.
    [3] Ching-Hon Pui, Siebold S. N. de Graaf, Lois W. Dow, John H. Rodman, William E. Evans, Bruce S. Alpert and Sharon B. Murphy. Phase I Clinical Trial of Orally Administered 4-Demethoxydaunorubicin (Idarubicin) with Pharmacokinetic and in Vitro Drug Sensitivity Testing in Children with Refractory Leukemia. Cancer Research. 1988, 48: 5348-5352.
- Properties
  - Alternative Name
    
    (7S,9S)-9-acetyl-7-(((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-6,9,11-trihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride
    
    CAS Number
    
    57852-57-0
    
    Molecular Formula
    
    C26H28ClNO9
    
    Molecular Weight
    
    533.95
    
    Purity
    
    99.86%
    
    Solubility
    
    ≥26.7 mg/mL in DMSO; insoluble in EtOH; ≥2.39 mg/mL in H2O with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Idarubicin HCl

Background

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