(1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[8.7.6]tricos-11-ene-2,5,8,19,22-pentone
128517-07-7 Basic informationMore
- Product Name:(1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[8.7.6]tricos-11-ene-2,5,8,19,22-pentone
- Synonyms: FK228 RoMidepsin 5)-disulfide Cyclo[(2Z)-2-aMino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-Mercapto-4-heptenoyl-D-valyl-D-cysteinyl],cyclic (3® (1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[8.7.6]tricos-11-ene-2,5,8,19,22-pentone RoMidepsin (FK228, Depsipeptide) Romidepsin Antibiotic FR 901228 Romidepsin, >=98% (1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[ FR 901228
- CAS:128517-07-7
- MF:C24H36N4O6S2
- MW:540.7
- EINECS:
- Mol File:128517-07-7.mol
USE
The U.S. FDA approved romidepsin (also referredto as FK228) in 2009 for
the treatment of cutaneous T-cell lymphoma (CTCL) for patients who
received at least one systemic therapy.
Romidepsin is a natural product that was
first isolated from the fermentation broth of C. violaceum. Romidepsin is the
second histone deacetylase (HDAC) inhibitor approved for CTCL, the other
being vorinostat,whichwas approved by the FDA in 2006. Unlike vorinostat
which is a pan-HDAC inhibitor, romidepsin shows modest selectivity for
class I HDACs in in vitro assays. It has been shown that after romidepsin
enters the cytoplasm, the disulfide bond is cleaved by glutathione to release
the sulfhydryl groupwhich chelateswith the activesite zinc of class IHDACs
and inhibits the enzymatic activity at nanomolar concentrations.
Although romidepsin inhibits class I HDACs, it is 17–23 times less potent as
the parent than the corresponding reduced form at each isozyme. For example,
the IC<sub>50</sub> of romidepsin at HDAC1 is 36±16nM while that of the reduced form is IC<sub>50</sub>=1.6± 0.9nM.Romidepsinhasalsobeenshownto induce cell cycle arrest, differentiation, and apoptosis in tumor cells by mechanisms
that cannot be completely explained by HDAC inhibition alone.Labelled Romidepsin (R425060). Romidepsin is a histone deacetylase inhibitor that can alter chromatin structure and gene transcription leading to multiple changes in cellular protein production. This
may result in cell cycle arrest and tumor growth inhibition. Romidepsin has shown anti-proliferative activity in vitro against multiple mouse and human tumor cell lines and in vivo in human tumor xeno
graft models. Romidepsin can be administered with a second agent, such as a cytotoxic agent, a steroidal agent, a proteasome inhibitor, or a kinase inhibitor.
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- Romidepsin
- US $1.00 /g
- CAS:128517-07-7
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 2000kg
- 2019-07-31
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- Products Intro:Product Name:RoMidepsin (FK228, Depsipeptide)
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