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KPT-276 CRM1 inhibitor

Name: KPT-276
Brand: Selleck Chemicals
SKU: S7251
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S7251

KPT-276 is an orally bioavailable selective CRM1 inhibitor.

Chemical Structure

Molecular Weight: 426.26

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

Quality Control

Batch: S725101 DMSO]20 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.45%

99.45

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) KPT-185 Verdinexor (KPT-335) Exportin-1/CRM1 Antibody [B23M5] Leptomycin B (LMB)

Chemical Information, Storage & Stability

Molecular Weight	426.26	Formula	C₁₆H₁₀F₈N₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1421919-75-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1C(CN1C(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)(F)F

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (46.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : 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.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.73mM)	Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. 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

Features	Superior oral bioavailability and PK profile relative to KPT-185 in vivo. Potential for use in hematological malignancies such as AML and multiple myeloma.
Targets/IC₅₀/Ki	CRM1 ^[1]
In vitro	KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. ^[2] This compound specifically and irreversibly inhibits the nuclear export function of XPO1, and reduces the viability of 12 HMCLs. It also actively induces apoptosis in primary MM patient samples. ^[3]
In vivo	KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. ^[1] This compound significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity. ^[2] It reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/22677130/ [2] https://pubmed.ncbi.nlm.nih.gov/22986101/ [3] https://pubmed.ncbi.nlm.nih.gov/23752175/

Tech Support

Handling Instructions

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

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