Eltanexor
Based on 3 publication(s) in Google Scholar
Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines.
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- Purity: 99.79%
- CAS No.: 1642300-52-4
- 화학식: C17H10F6N6O
- 분자량:428.29
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Eltanexor
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WB
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Cell Proliferation/Viability Assay
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RT-PCR
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WB
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IF
Biological Activity
XPO1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H9 | IC50 |
139.4 nM
Compound: KPT-8602
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Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
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[PMID: 35367710] |
| MM1.S | IC50 |
64 nM
Compound: KPT-8602
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Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
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[PMID: 35367710] |
| NAMALVA | IC50 |
93.8 nM
Compound: KPT-8602
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Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
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[PMID: 35367710] |
| YT | IC50 |
103.1 nM
Compound: KPT-8602
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Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay
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[PMID: 35367710] |
KPT-8602 (2-6 nM; 72 hours) reduces cell viability in leukemia cell lines with EC50s ranging from 25 to 145 nM[1].
KPT-8602 (1 nM; 16 hours) induces apoptosis in leukemia cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T-ALL cells (Jurkat, MOLT-4, ALL-SIL, DND41, and HPB-ALL), B-ALL cells (BV173, EHEB, and REH), AML cells (MV4-11, MOLM13, K-562, and HL-60)
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Concentration:2, 4, 6 nM
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Incubation Time:72 hours
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Result:Cell viability was reduced with EC50 values ranging from 25 to 145 nM.
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Cell Line:T-ALL, B-ALL, AML cells
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Concentration:1 μM
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Incubation Time:16 hours
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Result:Appearance of cleaved caspase-3 substrate PARP as early as 6 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (model with the JAK3 (M511I) mutation)[1]
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Dosage:15 mg/kg
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Administration:Oral gavage; daily for 12 days
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Result:Showed a marked reduction in total white blood cell (WBC) counts after 2 days of treatment compared to placebo-treated animals and the WBC counts continued to drop until they reached normal levels (<10,000 cells/μL) by day 12.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1642300-52-4
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Appearance Solid
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분자량 428.29
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화학식 C17H10F6N6O
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Color Off-white to light yellow
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SMILES
FC(F)(F)C1=CC(C(F)(F)F)=CC(C2=NN(/C=C(C3=CN=CN=C3)/C(N)=O)C=N2)=C1
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Synonyms
KPT-8602
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Front Microbiol
The Second-Generation XPO1 Inhibitor Eltanexor Inhibits Human Cytomegalovirus (HCMV) Replication and Promotes Type I Interferon Response. [Abstract]2021 May 3:12:675112. PMID: 34012430
Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]
Eltanexor (0.05-0.8 μM) inhibited the expression of IE2/86 (encoded by UL122), early protein pp52 (UL44), and late proteins pp71 and pp65 (UL82 and UL83) in a dose-dependent manner in HFFs infected with HCMV.
Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]
Eltanexor (0.05-0.8 μM) inhibited the production of HCMV progeny virions in a dose-dependent manner.
Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]
Eltanexor (0.4 μM; 36-96 h) increaseed the transcript levels of UL36, and reduced the transcript levels of UL122, E (UL44) and L (UL82, UL83, UL99, and UL75) genes in HFFs infected with HCMV.
Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]
Eltanexor (0.4 μM; 6-96 h) significantly reduced IE2, and suppressesed the protein levels of E protein pp52 (encoded by UL44), pp65 (UL83), pp71 (UL82), and L protein pp28 (UL99) after 36 hpi in HFFs infected with HCMV.
Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]
Eltanexor (0.4 μM) inhibited the nuclear export of the viral tegument protein pp65 in HFFs infected with HCMV.
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Exp Cell Res
KPT-8602 combined with IFN-γ released ZBP1-PANoptosome to inhibit the progression of primary central nervous system lymphoma. [Abstract]2026 Feb 18;457(2):114946. PMID: 41720446 -
BMC Cancer
Targeting EP300 in diffuse large b-cell lymphoma: efficacy of A485 and synergistic effects with XPO1 inhibition. [Abstract]2025 May 28;25(1):955. PMID: 40437414
용액&용해도
DMSO : ≥ 100 mg/mL (233.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.84 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3349 mL | 11.6743 mL | 23.3487 mL | 58.3717 mL |
| 5 mM | 0.4670 mL | 2.3349 mL | 4.6697 mL | 11.6743 mL | |
| 10 mM | 0.2335 mL | 1.1674 mL | 2.3349 mL | 5.8372 mL | |
| 15 mM | 0.1557 mL | 0.7783 mL | 1.5566 mL | 3.8914 mL | |
| 20 mM | 0.1167 mL | 0.5837 mL | 1.1674 mL | 2.9186 mL | |
| 25 mM | 0.0934 mL | 0.4670 mL | 0.9339 mL | 2.3349 mL | |
| 30 mM | 0.0778 mL | 0.3891 mL | 0.7783 mL | 1.9457 mL | |
| 40 mM | 0.0584 mL | 0.2919 mL | 0.5837 mL | 1.4593 mL | |
| 50 mM | 0.0467 mL | 0.2335 mL | 0.4670 mL | 1.1674 mL | |
| 60 mM | 0.0389 mL | 0.1946 mL | 0.3891 mL | 0.9729 mL | |
| 80 mM | 0.0292 mL | 0.1459 mL | 0.2919 mL | 0.7296 mL | |
| 100 mM | 0.0233 mL | 0.1167 mL | 0.2335 mL | 0.5837 mL |
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