Name: KPT-330
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    KPT-330, analog of KPT-185, is a selective inhibitor of CRM1 [1].
    Chromosomemaintenance protein 1 (CRM1) is a nuclear export receptor involved in the active transport of transcription factors, cell-cycle regulators, tumor suppressors and RNA molecules. In cancer, CRM1 is overexpression and overactive transport [1].
    KPT-330 is an orally bioavailable and selective CRM1 inhibitor. In kidney cancer (RCC) cells, KPT-330 inhibited CRM1 and increased nuclear localization of p21. Then, KPT-330 induced apoptosis and inhibited cells growth [2]. In human non-small cell lung cancer (NSCLC) cells, KPT-330 inhibited cell proliferation and induced the expression of apoptosis-related proteins and cell cycle arrest [3].
    In mice bearing MiaPaCa-2 xenograft model, KPT-330 (20 mg/kg) significantly inhibited tumor growth without significant toxicity or body weight loss. Also, KPT-330 increased PAR-4, pro-apoptotic Bax, cleaved PARP and caspase-3. These results suggested that KPT-330 induced apoptosis by the activation of PAR-4 signaling [1]. In mice bearing human NSCLC xenografts, KPT-330 significantly inhibited tumor growth [3].
    
    [1]. Azmi AS, Aboukameel A, Bao B, et al. Selective inhibitors of nuclear export block pancreatic cancer cell proliferation and reduce tumor growth in mice. Gastroenterology, 2013, 144(2): 447-456.
    [2]. Wettersten HI, Landesman Y, Friedlander S, et al. Specific inhibition of the nuclear exporter exportin-1 attenuates kidney cancer growth. PLoS One, 2014, 9(12): e113867.
    [3]. Sun H, Hattori N, Chien W, et al. KPT-330 has antitumour activity against non-small cell lung cancer. Br J Cancer, 2014, 111(2): 281-291.
- Properties
  - Alternative Name
    
    (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyrazin-2-ylprop-2-enehydrazide
    
    CAS Number
    
    1393477-72-9
    
    Molecular Formula
    
    C17H11F6N7O
    
    Molecular Weight
    
    443.31
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥11.52 mg/mL in EtOH; ≥15.15 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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