Eltanexor (KPT-8602)

Catalog No.S8397 Batch:S839704

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Technical Data

Formula

C17H10F6N6O
Molecular Weight 428.29 CAS No. 1642300-52-4
Solubility (25°C)* In vitro DMSO 29 mg/mL (67.71 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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]
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 Assay:

[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 Study:

[1]
  • Animal Models

    NOD-SCID-IL2Rcγnull (NSG) mice

  • Dosages

    15 mg/kg

  • Administration

    by oral gavage

Selleck's Eltanexor (KPT-8602) has been cited by 12 publications

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] PubMed: 38262581
The synergy of the XPO1 inhibitors combined with the BET inhibitor INCB057643 in high-grade B-cell lymphoma via downregulation of MYC expression [ Sci Rep, 2023, 13(1):18554] PubMed: 37899423
Eltanexor Effectively Reduces Viability of Glioblastoma and Glioblastoma Stem-Like Cells at Nano-Molar Concentrations and Sensitizes to Radiotherapy and Temozolomide [ Biomedicines, 2022, 10(9)2145] PubMed: 36140245
Prognostic and therapeutic significance of XPO1 in T-cell lymphoma [ Exp Cell Res, 2022, 416(2):113180] PubMed: 35489384
PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia [ J Hematol Oncol, 2021, 14(1):97] PubMed: 34167562
Targeting XPO1 enhances innate immune response and inhibits KSHV lytic replication during primary infection by nuclear stabilization of the p62 autophagy adaptor protein [ Cell Death Dis, 2021, 12(1):29] PubMed: 33414399
Combining selective inhibitors of nuclear export (SINEs) with chimeric antigen receptor (CAR) T cells for CD19‑positive malignancies [ Oncol Rep, 2021, 46(2)170] PubMed: 34165175
The XPO1 Inhibitor KPT-8602 Synergizes with Dexamethasone in Acute Lymphoblastic Leukemia [ Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-20-1315] PubMed: 32826328
Transcriptome Profiling of Acquired Gefitinib Resistant Lung Cancer Cells Reveals Dramatically Changed Transcription Programs and New Treatment Targets [ Front Oncol, 2020, 10:1424] PubMed: 32923394
[ J Hematol Oncol, 2019, ] PubMed: 31752970

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.