Plitidepsin
Based on 5 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.
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- Pureza: 99.94%
- No. CAS: 137219-37-5
- Fòrmula: C57H87N7O15
- Peso molecular:1110.34
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Plitidepsin
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Actividad biológica
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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] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 137219-37-5
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Appearance Solid
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Peso molecular 1110.34
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Fòrmula 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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Synonyms
Aplidine; PM90001
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Initial Source
Mediterranean tunicate Aplidium albicans
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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 (5)
Solvente y solubilidad
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.
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 (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.
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.
Pureza y Documentación
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Ficha de datos (287 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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Instrucciones de manejo (2659 KB)
Referencias
[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 |
|---|---|---|---|---|---|
| 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 Related Classifications
HY-16050 Related Classifications
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