Eltanexor (KPT-8602)

For research use only.

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

8 publications

Eltanexor (KPT-8602) Chemical Structure

CAS No. 1642300-52-4

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.

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

Purity & Quality Control

Choose Selective CRM1 Inhibitors

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.
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]

Methods Test Index PMID
Western blot

PubMed: 26654943     

MM.1S cells were treated with increasing concentrations of KPT-8602 followed by treatment with 0.1 μM biotinylated SINE compound and processed for the XPO1 occupancy assay. Digital western blot images for eluates and inputs as well as plots for the ratio 䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆà㺣痖뙠ෆ€𢡄뙤ෆ€䀷痗뙤ෆ౴뙤ෆ㵶痗뙤ෆ뺖᎒泌Itemセ᎒Count﫨呂뚔ෆ猴፲뙤ෆ፲씢痗猸፲髸莤䥷堙᎒セ᎒�堞ﻮ᎒፲露𢡄堚ю齃礤

p53 / NPM1; 

PubMed: 27323910     

Representative confocal microscopy images of p53 and NPM1 in MV4-11 and OCI-AML3 cells. The left panel shows the DAPI staining (cell nucleus). The middle panel is p53 and NPM1 staining and the right panel is the merger of p53 and NPM1 and DAPI staining.

p62 / p53 ; 

PubMed: 31088931     

Expression of p53 and p62 in AGS, HUH7, MM, and KMM cells after treatment with 1 µM KPT-8602 for 24 h analyzed by immunofluorescence assay. The sections were counterstained with DAPI, and pictures were taken with a confocal microscopy (magnification, ×600

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].


Cell Research:


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  • 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.

    (Only for Reference)
Animal Research:


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  • Animal Models: NOD-SCID-IL2Rcγnull (NSG) mice
  • Dosages: 15 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 428.29


CAS No. 1642300-52-4
Storage powder
in solvent
Synonyms ONO-7706,ATG-016
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

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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) Karyopharm Therapeutics Inc January 2016 Phase 1|Phase 2

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID