Eltanexor (KPT-8602)
目录号 : GC19466
Eltanexor (KPT-8602)是一种口服有效的输出蛋白-1（XPO1）抑制剂（EC50 = 60.9nM）。
Cas No.:1642300-52-4
Sample solution is provided at 25 µL, 10mM.
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Eltanexor (KPT-8602) is an orally active exportin-1 (XPO1) inhibitor (EC50 = 60.9nM) [1]. By inhibiting the nuclear export protein XPO1, Eltanexor leads to the nuclear accumulation of tumor suppressor proteins, restoring their tumor suppressor function and selectively inducing apoptosis in cancer cells [2-3]. Eltanexor is primarily used to treat multiple myeloma and acute leukemia [4].
In U87 cells, decreased cell viability after Eltanexor (1nM-10μM; 5d) treatment [5]. In HCT116 cells, Eltanexor (1nM-10μM; 72h) treatment reduces cancer cell viability cells [6].
In acute myeloid leukemia PDX2 mice model, Eltanexor (10mg/kg; ig; 4 weeks) treatment significantly reduced bioluminescence and prolonged survival of mice [7]. In recurrent clival chordoma mice model, Eltanexor (10mg/kg; po; 6 weeks) treatment significantly reduced tumor volume [8].
References:
[1]. Cornell R F, Rossi A C, Baz R, et al. Eltanexor (KPT-8602), a second-generation selective inhibitor of nuclear export (SINE) compound, in patients with refractory multiple myeloma[J]. Blood, 2017, 130: 3134.
[2]. Lai C, Xu L, Dai S. The nuclear export protein exportin‐1 in solid malignant tumours: From biology to clinical trials[J]. Clinical and Translational Medicine, 2024, 14(5): e1684.
[3]. Azizian N G, Li Y. XPO1-dependent nuclear export as a target for cancer therapy[J]. Journal of hematology & oncology, 2020, 13(1): 61.
[4]. Richard S, Jagannath S. Targeting nuclear export proteins in multiple myeloma therapy[J]. BioDrugs, 2022, 36(1): 13-25.
[5]. Otte K, Zhao K, Braun M, et al. Eltanexor Effectively Reduces Viability of Glioblastoma and Glioblastoma Stem-Like Cells at Nano-Molar Concentrations and Sensitizes to Radiotherapy and Temozolomide[J]. Biomedicines, 2022, 10(9): 2145.
[6]. Evans A E, Afroz S, Magstadt A, et al. The XPO1 inhibitor Eltanexor modulates the Wnt/β-catenin signaling pathway to reduce colorectal cancer tumorigenesis[J]. Cancer Research Communications, 2025.
[7]. Prolonged X P O. Prolonged XPO1 inhibition is essential for optimal antileukemic activity in NPM1-mutated AML[J]. 2022.
[8]. Walker C J, Chang H, Henegar L, et al. Selinexor inhibits growth of patient derived chordomas in vivo as a single agent and in combination with abemaciclib through diverse mechanisms[J]. Frontiers in Oncology, 2022, 12: 808021.
Eltanexor (KPT-8602)是一种口服有效的输出蛋白-1（XPO1）抑制剂（EC50 = 60.9nM） [1]。通过抑制核输出蛋白XPO1，Eltanexor导致肿瘤抑制蛋白在核内聚集，恢复其肿瘤抑制功能，并选择性诱导癌细胞凋亡 [2-3]。Eltanexor主要用于治疗多发性骨髓瘤和急性白血病 [4]。
在U87细胞中，Eltanexor（1nM-10μM；5d）治疗后细胞活力降低 [5]。在HCT116细胞中，Eltanexor（1nM-10μM；72h）治疗可降低癌细胞活力 [6]。
在急性髓性白血病PDX2小鼠模型中，Eltanexor（10mg/kg；ig；4周）治疗显著降低了小鼠的生物发光并延长了小鼠的生存期 [7]。在复发性斜坡脊索瘤小鼠模型中，Eltanexor（10mg/kg；po；6周）治疗显著缩小了肿瘤体积 [8]。
| Cell experiment [1]: | |
Cell lines | U87 cells |
Preparation Method | To evaluate cytotoxic effects, cells were seeded in 96-well plates 24h before treatment with Eltanexor, or DMSO as vehicle control. For seeding cells, the following cell densities were chosen: U87 cells. Twenty-four hours after plating, cells were treated with the indicated concentrations. As a control, (100% viability), the solvent DMSO was used in the concentration corresponding to the highest dose of Eltanexor. For U87 cells, cell viability was detected after five days. After 15min of mixing on a platform shaker and 15min of incubation at room temperature, both in the dark, luminescence was measured using a FLUOst. |
Reaction Conditions | 1nM-10μM; 5d |
Applications | Decreased cell viability after Eltanexor treatment. |
| Animal experiment [2]: | |
Animal models | Acute myeloid leukemia (AML) PDX2 mice model |
Preparation Method | Eight- to 10-week-old female NSG mice were intravenously injected with PDX2 cells stably transduced with the pHIV-Luc-ZsGreen vector. For survival experiments, PDX2 mice were divided into two treatment groups and given either vehicle or Eltanexor (10mg/kg, oral gavage) for four consecutive weeks. Body weight was monitored twice weekly, and leukemic cell engraftment was monitored weekly using bioluminescence. |
Dosage form | 10mg/kg; ig; 4 weeks |
Applications | Eltanexor treatment significantly reduced bioluminescence and prolonged survival of mice. |
References: | |
| Cas No. | 1642300-52-4 | SDF | |
| 化学名 | (E)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-2-(pyrimidin-5-yl)acrylamide | ||
| Canonical SMILES | FC(F)(F)C1=CC(C2=NN(/C=C(C3=CN=CN=C3)/C(N)=O)C=N2)=CC(C(F)(F)F)=C1 | ||
| 分子式 | C17H10F6N6O | 分子量 | 428.29 |
| 溶解度 | 85 mg/mL in DMSO(warmed with 50ºC water bath)；Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3349 mL | 11.6743 mL | 23.3487 mL |
| 5 mM | 467 μL | 2.3349 mL | 4.6697 mL |
| 10 mM | 233.5 μL | 1.1674 mL | 2.3349 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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