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MedKoo product information:

Elisidepsin

MedKoo Code#:  202300

Name:  Elisidepsin

CAS#:  681272-30-0

 

Synonym:   Brand name: Irvalec®. PM­02734

 

IUPAC/Chemical name: 

(2R)-N-((S)-5-amino-1-(((2R,3S)-1-(((3S,9S,12S,15R,18S,19R,Z)-9-benzyl-15-((S)-sec-butyl)-6-ethylidene-3,12-diisopropyl-19-methyl-2,5,8,11,14,17-hexaoxo-1-oxa-4,7,10,13,16-pentaazacyclononadecan-18-yl)amino)-3-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl)-1-((2R,5S,11R,16S)-8-((R)-1-hydroxyethyl)-2,5,11-triisopropyl-16-methyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazaoctadecan-1-oyl)pyrrolidine-2-carboxamide 2,2,2-trifluoroacetate

 

Chemical structure:

Theoretical analysis:

PM­02734 (trifluoroacetic acid, salt form)
Chemical Formula: C77H125F3N14O18
Molecular Weight: 1591.89
Elemental Analysis: C, 58.10; H, 7.91; F, 3.58; N, 12.32; O, 18.09

PM-02734 (free base form)
Chemical Formula: C75H124N14O16
Exact Mass: 1476.93197
Molecular Weight: 1477.87126
m/z: 1476.93197 (100.0%), 1477.93533 (81.1%), 1478.93868 (32.5%), 1479.94204 (8.5%), 1477.92901 (5.2%), 1478.93236 (4.2%), 1478.93622 (3.3%), 1479.93957 (2.7%), 1479.93572 (1.7%), 1480.94539 (1.7%), 1477.93825 (1.4%), 1478.94161 (1.2%), 1480.94293 (1.1%)
Elemental Analysis: C, 60.95; H, 8.46; N, 13.27; O, 17.32

 

Availability and price:

This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

 

Information about this agent

Elisidepsin is a marine-derived, synthetic cyclic depsipeptide with potential antineoplastic activity. Elisidepsin is a derivative of a natural marine compound that belongs to a family of dehydro aminobutyric acid-containing peptides (kahalalides) isolated from the herbivorous marine mollusk Elysia rufescens. Although the primary mechanism of action has yet to be elucidated, this agent exhibits anti-proliferative activity in a wide variety of cancer cell types, including breast, colon, pancreas, lung, and prostate; it appears to induce oncolytic rather than apoptotic cell death. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

 

Elisidepsin (PM02734) is a novel chemical entity resulting from PharmaMar's internal research program for derivatives of marine natural compounds. Produced synthetically in-house by PharmaMar, PM02734 is a new depsipeptide of the kahalalides family. Preliminary in vitro in-house studies identified PM02734 as a new antiproliferative drug demonstrating activity against a broad spectrum of tumor types: breast, colon, pancreas, lung and prostate, among others. PM02734 has been selected for clinical development based on its in vivo activity in xenografted human tumors, as well as an acceptable non-clinical toxicology profile. The new Phase I clinical trial of PM02734 is a multicenter, international (US and Europe) study designed to determine safety and tolerability and to identify the maximum tolerated dose (MTD) and recommended dose (RD) of PM02734 administered to patients with advanced malignant solid tumors.  (source: prnewswire).

 

Current developer:    PharmaMar Inc

 

References

1: Provencio M, Sánchez A, Gasent J, Gómez P, Rosell R. Cancer treatments: can we find treasures at the bottom of the sea? Clin Lung Cancer. 2009 Jul;10(4):295-300. Review. PubMed PMID: 19632950.

2: Ling YH, Aracil M, Jimeno J, Perez-Soler R, Zou Y. Molecular pharmacodynamics of PM02734 (elisidepsin) as single agent and in combination with erlotinib; synergistic activity in human non-small cell lung cancer cell lines and xenograft models. Eur J Cancer. 2009 Jul;45(10):1855-64. Epub 2009 Apr 5. PubMed PMID: 19346126; PubMed Central PMCID: PMC2700178.

3: Herrero AB, Astudillo AM, Balboa MA, Cuevas C, Balsinde J, Moreno S. Levels of SCS7/FA2H-mediated fatty acid 2-hydroxylation determine the sensitivity of cells to antitumor PM02734. Cancer Res. 2008 Dec 1;68(23):9779-87. PubMed PMID: 19047157.

4: Yin J, Aviles P, Lee W, Ly C, Guillen MJ, Munt S, Cuevas C, Faircloth G. Development of a liquid chromatography/tandem mass spectrometry assay for the quantification of PM02734, a novel antineoplastic agent, in dog plasma. Rapid Commun Mass Spectrom. 2006;20(18):2735-40. PubMed PMID: 16921565.

 

 

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