Home Transmembrane Transporters CRM1 inhibitor KPT-185 For research use only.

KPT-185

KPT-185 is a selective CRM1 inhibitor that induces growth inhibition and apoptosis in a panel of NHL cell lines with a median IC50 ~25 nM.

KPT-185 Chemical Structure

KPT-185 Chemical Structure

CAS No. 1333151-73-7

Purity & Quality Control

KPT-185 Related Products

Biological Activity

Description KPT-185 is a selective CRM1 inhibitor that induces growth inhibition and apoptosis in a panel of NHL cell lines with a median IC50 ~25 nM.
Targets
CRM1 [1]
In vitro
In vitro 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. [1] KPT-185 also inhibits proliferation and promotes apoptosis of pancreatic cancer cells without affecting human pancreatic ductal epithelial cells. [2]
Cell Research Cell lines AML cell lines (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1)
Concentrations ~10 μM
Incubation Time 72 hours
Method

Cells 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.

Chemical Information & Solubility

Molecular Weight 355.31 Formula

C16H16F3N3O3
CAS No. 1333151-73-7 SDF Download KPT-185 SDF
Smiles CC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (199.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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