유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재)
생식세포 변이원성 물질
구분 2
경고
P201,P202, P281, P308+P313, P405,P501
H410
장기적 영향에 의해 수생생물에 매우 유독함
수생 환경유해성 물질 - 만성
구분 1
경고
P273, P391, P501
예방조치문구:
P201
사용 전 취급 설명서를 확보하시오.
P202
모든 안전 조치 문구를 읽고 이해하기 전에는 취급하지 마시오.
P261
분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264
취급 후에는 손을 철저히 씻으시오.
P264
취급 후에는 손을 철저히 씻으시오.
P270
이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P272
작업장 밖으로 오염된 의복을 반출하지 마시오.
P273
환경으로 배출하지 마시오.
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P281
요구되는 개인 보호구를 착용하시오
P301+P310
삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P302+P352
피부에 묻으면 다량의 물로 씻으시오.
P308+P313
노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.
P321
(…) 처치를 하시오.
P330
입을 씻어내시오.
P333+P313
피부자극성 또는 홍반이 나타나면 의학적인 조치·조언를 구하시오.
P363
다시 사용전 오염된 의류는 세척하시오.
P391
누출물을 모으시오.
P405
밀봉하여 저장하시오.
P501
...에 내용물 / 용기를 폐기 하시오.
NFPA 704
0
2
0
(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 C화학적 특성, 용도, 생산
개요
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 IC50 of romidepsin at HDAC1 is 36±16nM while that of the reduced form is IC50=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.
화학적 성질
Pale Yellow Solid
용도
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.
정의
ChEBI: A cyclodepsipeptide consisting of the cyclic disulfide of (2Z)-2-aminobut-2-enoyl, L-valyl, (3S,4E)-3-hydroxy-7-sulfanylhept-4-enoyl, D-valyl and D-cystei
yl residues coupled in sequence and cyclised head-to tail.
Clinical Use
Romidepsin, a histone deacetylase inhibitor, originally developed by Fujisawa (now Astellas
Pharma), causes cell cycle arrest, differentiation, and apoptosis in various cancer cells. In 2004,
the FDA granted fast-track designation for romidepsin as monotherapy for the treatment of cutaneous Tcell
lymphoma (CTCL) in patients who have relapsed following, or become refractory to, other systemic
therapies. The FDA designated romidepsin as an orphan drug and it was approved in 2009 for this
indication and it was commercialized in 2010. In 2007, another fast-track designation was granted for
the product as monotherapy of previously treated peripheral T-cell lymphoma. Romidepsin (FR901228)
was originally discovered and isolated from the fermentation broth of Chromobacterium violaceum No.
968. It was identified through efforts in the search for novel agents which selectively reverse the
morphological phenotype of Ras oncogene-transformed cells since the Ras signaling pathway plays a
critical role in cancer development. Therefore, the drug could also have multiple molecular targets for
its anticancer activity besides HDAC. FR901228 is a bicyclic depsipeptide which is structurally
unrelated to any known class of cyclic peptides with an unusual disulfide bond connecting a thiol and Dcysteine.
(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 준비 용품 및 원자재
원자재
준비 용품
(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 공급 업체