| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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Plitidepsin (dehydrodemnin B; aplidine; Aplidin) is a naturally occurring cyclic depsipeptide extracted from the marine tunicate Aplidium albicans with a broad spectrum of anticancer activities.
| ln Vitro |
In MOLT-4 cells, plitidepsin (20 nM; 1 h) causes VEGF dependency [1]. In normal endothelial cells, which express VEGFR-1 but do not support VEGF, plitidepsin (20 nM; 1 h) does not significantly decrease VEGF-R1 mRNA [1]. SARS-CoV-2 is inhibited by plitidepsin, with an IC90 of 1.76 nM. Plitidepsin exhibits anti-SARS-CoV-2 action in hACE2-293T cells, with an IC90 of 0.88 nM. Plitidepsin suppresses SARS-CoV-2 replication in the established cell model of human lung cell samples, with an IC90 of 3.14 nM and a selectivity index of 40.4 [1].
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| ln Vivo |
In BALB/c samples expressing human ACE2, plitidepsin (ip; 0.3 mg/kg or 1 mg/kg; 2 hours prior to SARS-CoV-2 infection) dramatically lowers SARS-CoV-2 infection. In comparison to the vector desert, the SARS-CoV-2 viral decrease in the lungs was almost two log units lower in the 0.3 mg/kg plitidepsin group and 1.5 log units lower in the 1 mg/kg group [2].
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse[2]. 1]
Doses: 0.3 mg/kg; 1 mg/kg Dosing: 1 mg/kg QD for 1 day; 0.3 mg/kg daily for 3 days Experimental Results: Shown in vivo in SARS-CoV-2 infection mouse model Antiviral effect. |
| References |
[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.
[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. |
| Molecular Formula |
C57H87N7O15
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|---|---|
| Molecular Weight |
1110.34
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| Exact Mass |
1109.63
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| Elemental Analysis |
C, 61.66; H, 7.90; N, 8.83; O, 21.61
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| CAS # |
137219-37-5
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| Appearance |
Solid powder
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| SMILES |
CC[C@H](C)[C@@H]1[C@H](CC(=O)O[C@H](C(=O)[C@@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N([C@H](C(=O)O[C@@H]([C@@H](C(=O)N1)NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H]3CCCN3C(=O)C(=O)C)C)CC4=CC=C(C=C4)OC)C)CC(C)C)C)C(C)C)O
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| InChi Key |
UUSZLLQJYRSZIS-LXNNNBEUSA-N
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| InChi Code |
InChI=1S/C57H87N7O15/c1-15-33(8)46-44(66)29-45(67)79-49(32(6)7)48(68)34(9)50(69)58-39(26-30(2)3)54(73)64-25-17-19-41(64)56(75)62(13)43(28-37-20-22-38(77-14)23-21-37)57(76)78-36(11)47(52(71)59-46)60-51(70)42(27-31(4)5)61(12)55(74)40-18-16-24-63(40)53(72)35(10)65/h20-23,30-34,36,39-44,46-47,49,66H,15-19,24-29H2,1-14H3,(H,58,69)(H,59,71)(H,60,70)/t33-,34-,36+,39-,40-,41-,42+,43-,44-,46+,47-,49-/m0/s1
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| Chemical Name |
(2S)-N-[(2R)-1-[[(3S,6S,8S,12S,13R,16S,17R,20S,23S)-13-[(2S)-butan-2-yl]-12-hydroxy-20-[(4-methoxyphenyl)methyl]-6,17,21-trimethyl-3-(2-methylpropyl)-2,5,7,10,15,19,22-heptaoxo-8-propan-2-yl-9,18-dioxa-1,4,14,21-tetrazabicyclo[21.3.0]hexacosan-16-yl]amino]-4-methyl-1-oxopentan-2-yl]-N-methyl-1-(2-oxopropanoyl)pyrrolidine-2-carboxamide
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| Synonyms |
dehydrodemnin B; aplidine. US brand name: Aplidin.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~90.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.25 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9006 mL | 4.5031 mL | 9.0063 mL | |
| 5 mM | 0.1801 mL | 0.9006 mL | 1.8013 mL | |
| 10 mM | 0.0901 mL | 0.4503 mL | 0.9006 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05705167 | Recruiting | Drug: Plitidepsin | COVID-19 | PharmaMar | April 19, 2023 | Phase 2 |
| NCT02100657 | Completed | Drug: Plitidepsin Drug: Bortezomib |
Multiple Myeloma | PharmaMar | June 2014 | Phase 1 |
| NCT01149681 | Completed | Drug: APLIDIN (plitidepsin) |
Myelofibrosis | PharmaMar | July 2010 | Phase 2 |
| NCT00884286 | Completed | Drug: Aplidin® | Leukemia Lymphoma |
PharmaMar | December 2004 | Phase 2 |
| NCT00229203 | Completed | Drug: Plitidepsin | Multiple Myeloma | PharmaMar | February 2005 | Phase 2 |
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