product name KPT-185
Description: KPT-185 is a 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.
355.31
Formula
C16H16F3N3O3
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)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409220
| 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. Kinase Assay: 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 manufacturers protocol. The absorbance of wells at 450 nm (reference wavelength, 650 nm) is measured with a microplate reader. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Blood. 2012 Aug 30;120(9):1765-73; Gastroenterology. 2013 Feb;144(2):447-56. |
