Ceranib-2

- Overview
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    Background
    
    IC50: 28 μMCeranib-2 is an inhibitor of cellular ceramidase activity.
    Ceramidase catalyzes the hydrolysis of the N-acyl linkage between the fatty acid and sphingosine base in ceramide to produce sphingosine and a free fatty acid. Ceramidase plays a key role in regulating cell fate and its inhibition in both malignant and non-cancerous cells results in apoptosis.
    In vitro: In a previous study, a more potent analogue (Ceranib-2) of novel ceramidase inhibitor (Ceranib-1) was identified by screening a small molecule library. In a cell-based assay, both Ceranib-1 and Ceranib-2 were able to inhibit cellular ceramidase activity, decrease levels of sphingosine and S1P, inhibit the proliferation of cells alone and, induce the accumulation of multiple ceramide species, and induce cell-cycle arrest and death in combination with paclitaxel [1].
    In vivo: In a previous study, Ceranib-2 was given by i.p. injection on 5 days per week. Resutls showed that the average normalized size of tumors in each treatment group increased over time. However, by day 11 Ceranib-2-treated groups had significantly lower tumor volumes. By day 21, the average normalized tumor volumes for the control, 20 mg/kg and 50 mg/kg Ceranib-2 groups were 1,400, 940, and 710, respectively. In addition, the administration of Ceranib-2 did not alter the total body weight of the mice [1].
    Clinical trial: So far, no clinical study has been conducted.
    
    [1] Draper, J. M.,Xia, Z.,Smith, R.A., et al. Discovery and evaluation of inhibitors of human ceramidase. Molecular Cancer Therapeutics 1-27 (2011).
- Properties
  - Alternative Name
    
    3-[3-(4-methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
    
    CAS Number
    
    1402830-75-4
    
    Molecular Formula
    
    C25H19NO3
    
    Molecular Weight
    
    381.4
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Ceranib-2

Background

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