Eltanexor (KPT-8602)

Catalog No.S8397 Synonyms: Eltanexor

Eltanexor (KPT-8602) Chemical Structure

Molecular Weight(MW): 428.29

Eltanexor(KPT-8602) 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.

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Description Eltanexor(KPT-8602) 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]

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

Cell Research:

[2]

+ Expand
  • 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:

[1]

+ Expand
  • Animal Models: NOD-SCID-IL2Rcγnull (NSG) mice
  • Formulation: methylcellulose/tween 80
  • Dosages: 15 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL warmed (198.46 mM)
Ethanol 1 mg/mL warmed (2.33 mM)
Water Insoluble

* 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
Formula

C17H10F6N6O

CAS No. 1642300-52-4
Storage powder
in solvent
Synonyms Eltanexor

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02649790 Recruiting 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
NCT02649790 Recruiting 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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID