Eltanexor (KPT-8602)

製品コードS8397 バッチS839705

印刷

化学情報

Synonyms

ONO-7706，ATG-016

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇H₁₀F₆N₆O

分子量

428.29

CAS No.

1642300-52-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

22 mg/mL (51.36 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.150mg/ml (5.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 43 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Eltanexor (KPT-8602, ONO-7706，ATG-016) is a second-generation, orally bioavailable XPO1 inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure.
in vitro	Eltanexor (KPT-8602) is a potent inhibitor of AML cells in cell-based viability assays^[1]. It 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	Eltanexor (KPT-8602) is orally bioavailable and has similar pharmacokinetic properties to selinexor, but exhibits markedly reduced (approximately 30-fold less) penetration across the blood−brain barrier. Toxicology studies in rats and monkeys indicate that this compound 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. It also shows 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. It is minimally toxic to normal hematopoietic stem and progenitor cells^[1]. Additionally, it does not accumulate in plasma after repetitive dosing and prolongs survival in a human leukemia xenograft model of AML^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human CLL cells
	濃度	0-10 μM
	反応時間	24 h and 48 h
	実験の流れ	Eltanexor (KPT-8602) was evaluated using MTS assay and annexin-V/PI flow cytometry.
動物実験	動物モデル	NOD-SCID-IL2Rcγ^null (NSG) mice
	投薬量	15 mg/kg
	投与方法	by oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/27211268/
https://pubmed.ncbi.nlm.nih.gov/27323910/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Disparate leukemia mutations converge on nuclear phase-separated condensates [ Cell, 2025, S0092-8674(25)01149-3]	PubMed: 41192422
Targeting deubiquitinase USP7-mediated stabilization of XPO1 contributes to the anti-myeloma effects of selinexor [ J Transl Med, 2025, 23(1):62]	PubMed: 39806439
Inhibition of XPO1 by selinexor enhances terminal erythroid maturation through modulation of HSP70 trafficking in severe β0-thalassemia/HbE [ PLoS One, 2025, 20(9):e0333127]	PubMed: 40997022
Nuclear Phase Separation Drives NPM1-mutant Acute Myeloid Leukemia [ bioRxiv, 2025, 2025.05.23.655671]	PubMed: 40501735
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
A Novel Approach for Glioblastoma Treatment by Combining Apoptosis Inducers (TMZ, MTX, and Cytarabine) with E.V.A. (Eltanexor, Venetoclax, and A1210477) Inhibiting XPO1, Bcl-2, and Mcl-1 [ Cells, 2024, 13(7)632]	PubMed: 38607071
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。