Name: Pelitinib (EKB-569)
Price: 268.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Pelitinib (also known as EKB-569), a 3-cyanoquinoline, is a potent, and irreversible inhibitor of epidermal growth factor receptor (EGF-R) tyrosine kinase that inhibits the activity of EGF-R with the half maximal inhibition concentration IC50 value of 38.5 nM in vitro [1]. Pelitinib has been found to exert a potent anti-proliferative activity against tumor cells overexpressing EGF-R, including NHEK, A431 and MDA-468 cells, with IC50 values of 61 nM, 125 nM and 260 nM respectively; while it has also been found to potently inhibit EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells with IC50 values ranging from 20 nM to 80 nM [2].
    
    [1] Torrance CJ, Jackson PE, Montgomery E, Kinzler KW, Vogelstein B, Wissner A, Nunes M, Frost P, Discafani CM. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
    [2] Nunes M, Shi C, Greenberger LM. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.
- Properties
  - Alternative Name
    
    (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
    
    CAS Number
    
    257933-82-7
    
    Molecular Formula
    
    C24H23ClFN5O2
    
    Molecular Weight
    
    467.92
    
    Appearance
    
    A solid
    
    Purity
    
    98.49%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥11.7 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Pelitinib (EKB-569)

Pelitinib (EKB-569)

Background

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