Name: Eltanexor (KPT-8602)
Price: 215.00 USD

- Overview
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    Background
    
    Eltanexor (KPT-8602) is a second-generation, orally bioavailable inhibitor of exportin 1 (XPO1), with IC50 values of 20 ~ 211 nM in 10 acute myeloid leukemia (AML) cell lines. XPO1, also known as chromosome maintenance protein 1 (CRM1), is an important nuclear-cytoplasmic exporter in eukaryotes that transports a variety of protein cargoes from the nucleus to the cytoplasm, such as tumor suppressor proteins, cell cycle regulators and apoptosis inducers. Inhibition of XPO1-mediated nuclear export is a promising therapeutic strategy for many cancers, including chronic lymphocytic leukemia (CLL), AML, and aggressive lymphomas.
    
    1. Etchin J, Berezovskaya A, Conway AS, et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia, 2017, 31(1): 143-150.
    2. Hing ZA, Fung HY, Ranganathan P, et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia, 2016, 30(12): 2364-2372.
- Properties
  - Alternative Name
    
    (E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)acrylamide
    
    CAS Number
    
    1642300-52-4
    
    Molecular Formula
    
    C17H10F6N6O
    
    Molecular Weight
    
    428.29
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥44 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Eltanexor (KPT-8602)

Eltanexor (KPT-8602)

Background

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