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    KPT-185
    KPT-185

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1682
    CAS #: 1333151-73-7Purity ≥98%

    Description: This product has been discontinued. KPT-185 is a potent, irreversible and selective CRM1 inhibitor. In AML cell lines, KPT-185 inhibits proliferation of a variety of leukemia cells with IC50 values ranging from 100nM to 500nM. It induces cell-cycle arrest at G1 and induces apoptosis. KPT-185 also strongly affects cell colony formation. In addition, the inhibition of CRM1 caused by KPT-185 induces differentiation of AML blast. Besides that, KPT-185 is also found to inhibit proliferation and induce apoptosis of pancreatic cancer cells including Colo-357, HPAC and BxPC-3.

    References: Blood. 2012 Aug 30;120(9):1765-73; Gastroenterology. 2013 Feb;144(2):447-56.

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    Molecular Weight (MW)355.31
    FormulaC16H16F3N3O3
    CAS No.1333151-73-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 71 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: 71 mg/mL (199.8 mM)
    Solubility (In vivo) N/A
    Synonyms KPT-185; KPT185; KPT 185


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    In Vitro

    In vitro activity: KPT-185 significantly inhibits leukemia cell proliferation with IC50 ranging from 100 nM to 500 nM, and induces cell-cycle arrest and apoptosis of AML cell lines and primary AML blasts. KPT-185 reduces CRM1 protein protein level and shows a significant nuclear accumulation of CRM1 cargo proteins. KPT-185 also inhibits proliferation and promotes apoptosis of pancreatic cancer cells without affecting human pancreatic ductal epithelial cells. 


    Cell Assay: Cells [AML cell lines (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1)] are seeded into 96-well plates and treated for 24, 48, and 72 hours with KPT-SINE at various concentrations ranging from 10 nM to 10 μM. Cell viability is evaluated using the cell proliferation reagent WST-1 according to the manufacturer's protocol. The absorbance of wells at 450 nm (reference wavelength, 650 nm) is measured with a microplate reader.

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    References

    Blood. 2012 Aug 30;120(9):1765-73; Gastroenterology. 2013 Feb;144(2):447-56.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    KPT-185

    KPT SINEs induce cancer cell selective growth inhibition and apoptosis. Gastroenterology. 2013 Feb;144(2):447-56.
     
     

    KPT-185

    KPT-185 induces nuclear localization of different TSPs including PAR-4 in cancer selective manner. Gastroenterology. 2013 Feb;144(2):447-56.


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