Name: CYC116
Price: 180.00 USD

- Overview
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    Background
    
    IC50: 44 and 19 nM respectively for Aurora A and B in cancer cells
    Ki: 8.0 and 9.2 nM for aurora A and B, respectively
    The aurora kinases are a family of serine-threonine kinases that interact with components of the mitotic apparatus and that regulate aspects of centrosome maturation, bipolar spindle assembly, chromosome segregation, and cytokinesis. CYC116 has been discoverd as a novel N-phenyl-4-(thiazol-5-yl) pyrimidin-2-amine aurora kinase inhibitor.
    In vitro: The anticancer effects of CYC116 were shown to emanate from cell death following mitotic failure and increased polyploidy as a consequence of cellular inhibition of aurora A and B kinases. Moreover, CYC116 was also assessed against other kinases [1].
    In vivo: Preliminary in vivo assessment showed that CYC116 was orally bioavailable and possessed anticancer activity. The mean relative tumor volumes of mice receiving CYC116 at both dose levels were less than those of vehicle-treated mice for the duration of the study period [1].
    Clinical trials: CYC116 is currently undergoing evaluation in Phase I clinical trials.
- Properties
  - Alternative Name
    
    4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine
    
    CAS Number
    
    693228-63-6
    
    Molecular Formula
    
    C18H20N6OS
    
    Molecular Weight
    
    368.46
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥18.4 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CYC116

CYC116

Background

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