| 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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