elisidepsin

Names

[ CAS No. ]:
681272-30-0

[ Name ]:
elisidepsin

[Synonym ]:
(4S)-MeHex-D-Val-Thr-Val-D-Val-D-Pro-Orn-D-allo-Ile-cyclo(D-allo-Thr-D-allo-Ile-D-Val-Phe-Z-Dhb-Val)
isokahalalide F
(4S)-methylhexanoic kahalalide F
Elisidepsin

Biological Activity

[Description]:

Elisidepsin (PM02734) is cyclic depsipeptide with antineoplastic activity. Elisidepsin inhibits cancer cell proliferation. Elisidepsin can be used in the research of cancers, such as NSCLC[1][2][3][4].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[In Vitro]

Elisidepsin (72 h) inhibits various cancer cells proliferation with IC50s ranging from 0.4 μM (ZR-75-1) to 8.8 μM (MiaPaCa2)[1]. Elisidepsin (1 μM, 48 h) arrests SKBR3 cell in sub-G1 phase[1]. Elisidepsin (0-5 μM, 30 min) induces loss of cell membrane integrity in DU145 cells, instead of apoptosis[1]. Elisidepsin interacts with glycosylated ceramides in the plasma cell membrane of HCT-116 cells[2]. Elisidepsin (0.1 μM, 2 h) is effective in the induction of ErbB3 degradation and dephosphorylation in H322, A549 and H3255 cells[4]. Elisidepsin (0.5 and 1 μM, 2 h) inhibits the phosphorylation of ErbB3 and AKT in H322 cells and A549 cells[4]. Cell Viability Assay[1] Cell Line: SKBR3 cell Concentration: 0.125, 0.25, 0.5, 1 μM Incubation Time: 48 h Result: Increased amount of dying cells represented by sub-G1 phase.

[In Vivo]

Elisidepsin (100 µg/kg, i.v.) shows antitumor activity against lung cancer xenografts[3]. Animal Model: NSCLC xenograft models (A549 cell, i.v.) in nude mice[3] Dosage: 100 µg/kg Administration: Intravenous injection (i.v.) Result: Prolonged the life-span of animals bearing experimental lung metastases.

Chemical & Physical Properties

[ Molecular Formula ]:
C75H124N14O16

[ Molecular Weight ]:
1477.87000

[ Exact Mass ]:
1476.93000

[ PSA ]:
442.06000

[ LogP ]:
6.85490


Related Compounds