Name: Aurora A Inhibitor I
Price: 260.00 USD

- Overview
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    Background
    
    IC50: 3.4 nM.Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A . Aurora kinases are reported to be required for mitosis and to complete cell division. Because of this, Aurora kinase inhibitors have been investigated extensively as potential anticancer therapeutic agents. The two major Aurora kinases (Aurora A and Aurora B) are closely related in kinase domain sequence (71% identical).In vitro: Aurora A Inhibitor I was tested against wild-type kinase and two mutants (Aurora A (T217E) and Aurora B (E161T)). The inhibitory potencies of Aurora A Inhibitor I was strongly affected by the single amino acid substitutions. For either Aurora kinase, the presence of threonine allowed potent inhibition, while for glutamic acid variants, there was a approximately 100-fold shift in IC50, which supported the “gating” role for this residue. The Aurora B binding pocket was enlarged by the E161T mutation, while the pocket in Aurora A was closed by the T217E mutation. Aurora A Inhibitor I was exceptionally selective Aurora A inhibitors, as shown by no inhibition on Aurora B or CDKs was observed in cellular assays [1]. In vivo: So far, there is no animal in vivo study reported. Clinical trial: N/A
- Properties
  - Alternative Name
    
    N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]anilino]-5-fluoropyrimidin-4-yl]amino]benzamide
    
    CAS Number
    
    1158838-45-9
    
    Molecular Formula
    
    C31H31ClFN7O2
    
    Molecular Weight
    
    588.07
    
    Appearance
    
    A solid
    
    Purity
    
    98.83%
    
    Solubility
    
    ≥29.4 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Aurora A Inhibitor I

Aurora A Inhibitor I

Background

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