Home Transmembrane Transporters CRM1 inhibitor Eltanexor (KPT-8602)

Eltanexor (KPT-8602)

Catalog No.S8397 Synonyms: ONO-7706，ATG-016

For research use only.

Eltanexor (KPT-8602, ONO-7706，ATG-016) is a second-generation, orally bioavailable XPO1 (also known as CRM1) inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure.

Eltanexor (KPT-8602) Chemical Structure

CAS No. 1642300-52-4

Selleck's Eltanexor (KPT-8602) has been cited by 8 Publications

Purity & Quality Control

Choose Selective CRM1 Inhibitors

Related Compound Libraries

Biological Activity

Description Eltanexor (KPT-8602, ONO-7706，ATG-016) is a second-generation, orally bioavailable XPO1 (also known as CRM1) inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure.
Targets
XPO1 [1]
In vitro

KPT-8602 is a potent inhibitor of AML cells in cell-based viability assays[1]. KPT-8602 inhibits XPO1/cargo interactions and nuclear export, induces apoptosis of primary CLL cells and significantly inhibits proliferation of diffuse large B-cell lymphoma cell lines[2]
Assay
Methods Test Index PMID
Western blot XPO1 26654943
Immunofluorescence p53 / NPM1 ; p62 / p53 27323910 31088931
In vivo KPT-8602 is orally bioavailable and has similar pharmacokinetic properties to selinexor, but has markedly reduced (approximately 30-fold less) penetration across the blood−brain barrier. Toxicology studies in rats and monkeys indicate that KPT-8602 has a substantially better tolerability profile, probably due to its inability to penetrate into the CNS, with reduced anorexia, malaise and weight loss compared to selinexor. KPT-8602 exhibits superior anti-leukemic activity and better tolerability in the AML PDX models tested, with nearly complete elimination of human AML cells in the AML-CN model. KPT-8602 is minimally toxic to normal hematopoietic stem and progenitor cells[1]. KPT-8602 does not accumulate in plasma after repetitive dosing and prolongs survival in a human leukemia xenograft model of AML[2].

Protocol (from reference)

Cell Research:

[2]
  • Cell lines: Human CLL cells
  • Concentrations: 0-10 μM
  • Incubation Time: 24 h and 48 h
  • Method:

    MTS assay and annexin-V/PI flow cytometry.
Animal Research:

[1]
  • Animal Models: NOD-SCID-IL2Rcγnull (NSG) mice
  • Dosages: 15 mg/kg
  • Administration: by oral gavage

Solubility (25°C)

In vitro

 DMSO 85 mg/mL warmed
(198.46 mM)
Water Insoluble
Ethanol '1 mg/mL warmed

Chemical Information

Molecular Weight 428.29
Formula

C17H10F6N6O
CAS No. 1642300-52-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=C(C=C(C=C1C(F)(F)F)C(F)(F)F)C2=NN(C=N2)C=C(C3=CN=CN=C3)C(=O)N

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02649790 Recruiting Drug: KPT-8602|Drug: ASTX727|Drug: Dexamethasone Relapsed/Refractory Multiple Myeloma (RRMM)|Metastatic Colorectal Cancer (mCRC)|Metastatic Castration Resistant Prostate Cancer (mCRPC)|Higher Risk Myelodysplastic Syndrome (HR-MDS)|Acute Myeloid Leukemia (AML)|Newly Diagnosed Intermediate/High-Risk MDS Karyopharm Therapeutics Inc January 2016 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Eltanexor (KPT-8602) | Eltanexor (KPT-8602) supplier | purchase Eltanexor (KPT-8602) | Eltanexor (KPT-8602) cost | Eltanexor (KPT-8602) manufacturer | order Eltanexor (KPT-8602) | Eltanexor (KPT-8602) distributor