Home Transmembrane Transporters CRM1 inhibitor Eltanexor (KPT-8602) For research use only.

Eltanexor (KPT-8602)

Synonyms: ONO-7706，ATG-016

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

Eltanexor (KPT-8602) Chemical Structure

CAS No. 1642300-52-4

Purity & Quality Control

Eltanexor (KPT-8602) Related Products

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
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot XPO1 26654943
Immunofluorescence p53 / NPM1 p62 / p53 27323910
In Vivo
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].
Animal Research Animal Models NOD-SCID-IL2Rcγnull (NSG) mice
Dosages 15 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05918055 Recruiting
Myelodysplastic Syndromes
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 November 14 2023 Phase 1|Phase 2
NCT02649790 Active not recruiting
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

Chemical Information & Solubility

Molecular Weight 428.29 Formula

C17H10F6N6O
CAS No. 1642300-52-4 SDF Download Eltanexor (KPT-8602) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 85 mg/mL ( (198.46 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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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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