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KPT-185 CRM1 inhibitor

Name: KPT-185
Brand: Selleck Chemicals
SKU: S7125
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S7125

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.

Chemical Structure

Molecular Weight: 355.31

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.12%

99.12

Related Targets	CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel MCT Amino acid transporter GLUT VDAC BCRP NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
Related Products	Eltanexor (KPT-8602) Verdinexor (KPT-335) KPT-276 Exportin-1/CRM1 Antibody [B23M5] Leptomycin B (LMB)

Chemical Information, Storage & Stability

Molecular Weight	355.31	Formula	C₁₆H₁₆F₃N₃O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1333151-73-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (199.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.550mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 71 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (3.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound reduces CRM1 protein protein level and shows a significant nuclear accumulation of CRM1 cargo proteins. ^[1] It also inhibits proliferation and promotes apoptosis of pancreatic cancer cells without affecting human pancreatic ductal epithelial cells. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/22677130/ [2] https://pubmed.ncbi.nlm.nih.gov/23089203/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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