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 9 Publications

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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

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

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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)|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 2022-08-01)

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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