KPT-185

Catalog No.S7125

For research use only.

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

CAS No. 1333151-73-7

Selleck's KPT-185 has been cited by 7 Publications

1 Customer Review

Purity & Quality Control

Choose Selective CRM1 Inhibitors

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

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Solubility (25°C)

In vitro

DMSO 71 mg/mL
(199.82 mM)
Ethanol 71 mg/mL
(199.82 mM)
Water Insoluble

Chemical Information

Molecular Weight 355.31
Formula

C16H16F3N3O3

CAS No. 1333151-73-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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