Eltanexor Z-isomer
Based on 1 publication(s) in Google Scholar
Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 95.98%
- CAS No.: 1642300-78-4
- 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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- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Eltanexor Z-isomer
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Cell Proliferation/Viability Assay
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | EC50 |
9 nM
Compound: 17; KPT-8602
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Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay
Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay
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[PMID: 39005064] |
Chemical Information
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CAS No. 1642300-78-4
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Appearance Solid
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분자량 428.29
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화학식 C17H10F6N6O
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Color Light yellow to yellow
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SMILES
O=C(N)/C(C1=CN=CN=C1)=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2
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Synonyms
KPT-8602 (Z-isomer)
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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 (1)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
XPO1 intensifies sorafenib resistance by stabilizing acetylation of NPM1 and enhancing epithelial-mesenchymal transition in hepatocellular carcinoma. [Abstract]2023 Apr:160:114402. PMID: 36791564
Eltanexor Z-isomer purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Apr:160:114402. [Abstract]
A combination of sorafenib and KPT-8602 (30 mg/kg/day; 27 days) has a better tumor inhibition effect than sorafenib alone in xenograft tumor mice model (Fig. A-C).
용액&용해도
DMSO : 50 mg/mL (116.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.75 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Vercruysse T et al. The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. Clin Cancer Res. 2016 Oct 25. [Content Brief]
[2]. Hing ZA et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Jun 21. [Content Brief]
[3]. Etchin J et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia. 2016 Jun 24. [Content Brief]
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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