Clofarabine

- Overview
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    Background
    
    Clofarabine is a DNA synthesis inhibitor and a substrate of Deoxycytidine kinase (dCK).DCK is a key cytosolic enzyme in the DNA-synthesis salvage pathway and is responsible for the phosphorylation of clofarabine.Clofarabine is phosphorylated to form clofarabine triphosphate, which competes with dATP for DNA polymerase-α and -ε. At the same time, clofarabine-monophosphate is incorporated into internal and terminal DNA sites, which impaired DNA elongation and repair. Clofarabine triphosphate inhibits ribonucleotide reductase with IC50 value of 65 nM, which then reduced dCTP and dATP. Clofarabine is efficiently transported into cells through nucleoside transporters hENT1, hENT2, and hCNT2. Clofarabine results in release of cytochrome c, apoptosis protease-activating factor 1 (APAF1), apoptotic-inducing factor (AIF) and caspase 9 into the cytosol. In both rapidly growing and quiescent tumours, clofarabine has anticancer activity because of its inhibition of DNA synthesis and induction of apoptosis. Implanted human tumour xenografts in athymic nude or severe combined immune deficiency mice, Clofarabine administered intraperitoneally had significant antitumor activity.
    
    [1]. Bonate PL, Arthaud L, Cantrell WR Jr, et al. Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat Rev Drug Discov, 2006, 5(10): 855-863.
- Properties
  - Alternative Name
    
    (2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol
    
    CAS Number
    
    123318-82-1
    
    Molecular Formula
    
    C10H11ClFN5O3
    
    Molecular Weight
    
    303.68
    
    Appearance
    
    A solid
    
    Purity
    
    99.46%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥15.18 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Clofarabine

Background

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