Plitidepsin
Based on 6 publication(s) in Google Scholar
Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM). Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.91%
- CAS 番号: 137219-37-5
- 分子式: C57H87N7O15
- 分子量:1110.34
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保管条件:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Plitidepsin
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
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Bio/Physico-chemical Assay
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IHC
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.2 nM
Compound: 2
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Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 3 days
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 3 days
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[PMID: 33592144] |
| HT-29 | IC50 |
0.5 nM
Compound: 2
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Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 3 days
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 3 days
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[PMID: 33592144] |
| P388 | IC50 |
>1 μM
Compound: 2
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Inhibition of RNA synthesis in mouse P388 cells measured after 72 hrs
Inhibition of RNA synthesis in mouse P388 cells measured after 72 hrs
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[PMID: 33592144] |
| P388 | IC50 |
0.1 μM
Compound: 2
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Inhibition of DNA synthesis in mouse P388 cells measured after 72 hrs
Inhibition of DNA synthesis in mouse P388 cells measured after 72 hrs
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[PMID: 33592144] |
| P388 | IC50 |
0.2 nM
Compound: 2
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Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition incubated for 3 days
Antiproliferative activity against mouse P388 cells assessed as cell growth inhibition incubated for 3 days
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[PMID: 33592144] |
| P388 | IC50 |
0.5 μM
Compound: 2
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Inhibition of protein synthesis in mouse P388 cells measured after 72 hrs
Inhibition of protein synthesis in mouse P388 cells measured after 72 hrs
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[PMID: 33592144] |
| SK-MEL-28 | IC50 |
0.5 nM
Compound: 2
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 3 days
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 3 days
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[PMID: 33592144] |
| Vero C1008 | EC50 |
0.7 nM
Compound: Plitidepsin
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Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth
Antiviral activity against SARS-CoV-2 infected in African green monkey Vero E6 cells assessed as reduction in cell growth
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[PMID: 37229831] |
体外実験
Plitidepsin (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells[1]. Plitidepsin (20 nM; 1 h) does not result in significant inhibition of VEGF-R1 mRNA in normal endothelial cells, which do express VEGFR-1 but do not secrete VEGF[1]. Plitidepsin inhibits SARS-CoV-2 with an IC90 of 1.76 nM. In hACE2-293T cells, Plitidepsin exhibits anti-SARS-CoV-2 activity with an IC90 of 0.88 nM. In an established model of human pneumocyte-like cells, Plitidepsin inhibits SARS-CoV-2 replication with an IC90 of 3.14 nM and a selectivity index of 40.4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice[1]
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Dosage:0.3 mg/kg; 1 mg/kg
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Administration:1 day QD at 1 mg/kg; 3days QD at 0.3 mg/kg
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Result:Showed in vivo antiviral efficacy in mouse models of SARS-CoV-2 infection.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 137219-37-5
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性状 Solid
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分子量 1110.34
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分子式 C57H87N7O15
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Color White to off-white
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SMILES
O=C([C@@H](NC([C@H](C([C@@H](OC(C[C@@H]1O)=O)C(C)C)=O)C)=O)CC(C)C)N(CCC2)[C@]2([H])C(N([C@H](C(O[C@@H]([C@@H](C(N[C@]1([H])[C@@H](C)CC)=O)NC([C@@H](CC(C)C)N(C)C([C@H](CCC3)N3C(C(C)=O)=O)=O)=O)C)=O)CC(C=C4)=CC=C4OC)C)=O
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別名
Aplidine; PM90001
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Initial Source
Mediterranean tunicate Aplidium albicans
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Plitidepsin purchased from MedChemExpress. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2026 Jul 11.
U87 and U251 glioma cells were treated with Plitidepsin (0, 20, 40, 60 nM) for 12, 24, and 48 h. Cell viability was assessed using the CCK-8 assay. The results showed that Plitidepsin treatment significantly reduced cell viability in both U87 and U251 cells in a dose- and time-dependent manner.
Plitidepsin purchased from MedChemExpress. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2026 Jul 11.
U87 and U251 cells were treated with Plitidepsin (0, 20, 40, 60 nM) for 24 h, and cellular death was assessed by flow cytometry using Annexin V and PI staining. The results showed that Plitidepsin increased apoptosis in glioma cells in a dose-dependent manner.
Plitidepsin purchased from MedChemExpress. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2026 Jul 11.
Western blot analysis of pro-caspase-3 and cleaved caspase-3 levels in U87 and U251 cells treated with Plitidepsin (20, 40, 60 nM) for 24 h. Tubulin was used as a loading control. Western blot analysis demonstrated that Plitidepsin treatment induced the cleavage of pro-caspase-3 into its active form in glioma cells.
Plitidepsin purchased from MedChemExpress. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2026 Jul 11.
Caspase-3 activity was measured in U87 and U251 cells treated with Plitidepsin (0, 20, 40, 60 nM) for 24 h. The results showed that Plitidepsin increased the caspase-3 activities in a dose-dependent manner in glioma cells.
Plitidepsin purchased from MedChemExpress. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2026 Jul 11.
Representative IHC images (400 ×) showing reduced BMI1 expression and Ki-67 proliferation index in Plitidepsin (0.5 mg/kg-2 mg/kg; i.v.; every 3 days for 2 weeks)-treated tumors. Scale bars: 50 μm. Immunohistochemical analysis revealed reduced BMI1 expression and decreased proliferation (Ki-67 + cells) in Plitidepsin-treated tumors.
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Plitidepsin purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 27.
Cells were infected for 2 h with rHRSV-mCherry at MOI 0.2 and the medium was then replaced to incubate cells in the presence of serial dilutions of Plitidepsin for 48 h (red curve). The viral replication was quantified by measurement of the mCherry fluorescence. In parallel, cell viability upon treatment with Plitidepsin was quantified in non-infected HEp-2 cells (black curve). Plitidepsin inhibited rHRSV197 mCherry replication in a dose-dependent manner, with an IC50 of 3.5 nM.
Plitidepsin purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 27.
Representative images of HEp-2 cell cultures infected with rHRSV-mCherry at MOI 0.2, 48 hours post-infection in the absence or presence of Plitidepsin at 12, 4, and 1.4 nM. Nuclei were colored with Hoechst 33432. Scale bars, 250 µm.
Plitidepsin purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 27.
BSRT7 cells were transfected with the complete minigenome system or with the pEGFP plasmid coding for EGFP. Six hours later, the transfection mix was removed and medium containing Plitidepsin at different concentrations was added. Then, 24 h post-transfection, cells were lysed and analyzed by Western blotting using anti-N, anti-GFP or anti-alpha tubulin antibodies.
Plitidepsin purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 February 27.
BSRT7/5 cells were transfected with plasmids encoding the N, P, M2–1, and L proteins; the pMT/Luc minigenome, together with pCMV-beta-gal for transfection standardization. Serial dilutions of Plitidepsin were added 6 h post-transfection after removing transfection reagents. Viral RNA synthesis was quantified by measuring the luciferase activity after cell lysis 24 h post-transfection. Each luciferase minigenome activity value was normalized based on DMSO treated cells and is the average of three independent experiments performed in triplicate. Error bars represent standard deviations calculated based on three independent experiments made in triplicate.
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溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (90.06 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (2.25 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 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
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.
プロトコル
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
純度とドキュメンテーション
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データシート (287 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Alejandro Losada, et al. Translation Elongation Factor eEF1A2 is a Novel Anticancer Target for the Marine Natural Product Plitidepsin. Sci Rep. 2016 Oct 7;6:35100. [Content Brief]
[2]. Kris M White, et al. Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A. Science. 2021 Feb 26;371(6532):926-931. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9006 mL | 4.5031 mL | 9.0063 mL | 22.5156 mL |
| 5 mM | 0.1801 mL | 0.9006 mL | 1.8013 mL | 4.5031 mL | |
| 10 mM | 0.0901 mL | 0.4503 mL | 0.9006 mL | 2.2516 mL | |
| 15 mM | 0.0600 mL | 0.3002 mL | 0.6004 mL | 1.5010 mL | |
| 20 mM | 0.0450 mL | 0.2252 mL | 0.4503 mL | 1.1258 mL | |
| 25 mM | 0.0360 mL | 0.1801 mL | 0.3603 mL | 0.9006 mL | |
| 30 mM | 0.0300 mL | 0.1501 mL | 0.3002 mL | 0.7505 mL | |
| 40 mM | 0.0225 mL | 0.1126 mL | 0.2252 mL | 0.5629 mL | |
| 50 mM | 0.0180 mL | 0.0901 mL | 0.1801 mL | 0.4503 mL | |
| 60 mM | 0.0150 mL | 0.0751 mL | 0.1501 mL | 0.3753 mL | |
| 80 mM | 0.0113 mL | 0.0563 mL | 0.1126 mL | 0.2814 mL |
Plitidepsin 関連分類
HY-16050 関連分類
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