Romidepsin|128517-07-7|(罗米地辛; FK 228; FR 901228; NSC 630176)-陌孚医药/Medlife

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Romidepsin (Synonyms: 罗米地辛; FK 228; FR 901228; NSC 630176)

目录号: PL04359 纯度: ≥99%

CAS No. :128517-07-7

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中文名称	Romidepsin
中文别名	罗米地辛;2,2',3,4,4',5,5'-七溴联苯;Romidepsin (FK228, Depsipeptide) 抑制剂;罗米迪司肽;罗米地辛标准品;FK228 罗米地辛;罗米地辛, 一种有效的HDAC1和HDAC2抑制剂
英文名称	Romidepsin
英文别名	Romidepsin (FK228, Depsipeptide);(1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone;Cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl],cyclic (3®FK 228;FR-901228;Romidepsin;Romidepsin (depsipeptide,FK228, FR901228, NSC 630176,Istodax®);Romidepsin（FK228）;Chromadax;Depsipeptide;FK-228;FR 901228;Istodax;NSC 630176;Cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-(3S,4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl] cyclic (35)-disulfide;L-Valine, N-((3S,4E)-3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-D-valyl-D-cysteinyl-(2Z)-2-amino-2-butenoxyl-, (4-1)-lactone, cyclic (1-2)-disulfide;Antibiotic FR 901228;RoMidepsin-d8;FK228;FR901228;5)-disulfide;CX3T89XQBK;Romidepsin [USAN:INN];DSSTox_RID_82777;DSSTox_CID_28505;DSSTox_GSID_48579;L-Valine, N-(3-hydroxy-7-mercapto-1-oxo-4-heptenyl)-D-valyl-D-cysteinyl-(Z)-2,3-didehydro-2-aminobutanoyl-, xi-lactone, cyclic (1-2)-disulfide, (S-(E))-;L-Va;(1S,7Z,10S,16E,21R)-7-Ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone;Tox21_112907
Cas No.	128517-07-7
分子式	C₂₄H₃₆N₄O₆S₂
分子量	540.70
包装储存	Powder -20°C 3 years该产品在溶液状态不稳定，建议您现用现配，即刻使用。

产品详情

Romidepsin (FK 228) 是具有抗肿瘤活性的组蛋白去乙酰化酶 (HDAC) 抑制剂，抑制 HDAC1，HDAC2，HDAC4 和 HDAC6，IC₅₀ 值分别为 36 nM，47 nM，510 nM 和 1.4 μM。Romidepsin (FK 228) 由紫色杆菌产生，诱导 G2/M 细胞周期阻滞和凋亡 (apoptosis)。

生物活性

Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC 50 s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.

性状

Solid

IC50 & Target[1][2]

HDAC1 36 nM (IC50) HDAC2 47 nM (IC50

体外研究(In Vitro)

Romidepsin (0-72 hours; 0-80 nM) inhibits proliferation of HCC cells in dose-dependent manner.
Romidepsin (0-48 hours; 0-60 nM) leads to a time- and dose-dependent induction of cell cycle arrest in the G2/M phase in HCC cells.
Romidepsin (0-48 hours; 0-60 nM) promotesapoptosis in HCC cells, increases c-caspase-3, c-caspase-9, and c-PARP protein expression.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Romidepsin (intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days) inhibited the tumor growth, reveals a higher expression of p-cdc25C, ki67, c-caspase-3 and c-PARP, and a lower expression of Ki-67 in Romidepsin treated tumors . has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years该产品在溶液状态不稳定，建议您现用现配，即刻使用。

ClinicalTrial

参考文献

[1]. Furumai R, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 Sep 1;62(17):4916-21.
[2]. Sun WJ, et al. Romidepsin induces G2/M phase arrest via Erk/cdc25C/cdc2/cyclinB pathway and apoptosis induction through JNK/c-Jun/caspase3 pathway in hepatocellular carcinoma cells. Biochem Pharmacol. 2017 Mar 1;127:90-100.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (184.95 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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