产品名称

英文名称：Romidepsin (FK228, Depsipeptide)

同义词

Romidepsin、Istodax、Depsipeptide、Chromadax、FK228、128517-07-7、Antibiotic FR 901228、FR901228、FK 228、FK-228、FR 901228、NSC-630176、FR-901228、romidepsina、romidepsine、romidepsinum、NSC 630176、CHEBI61080、CX3T89XQBK、CHEMBL343448、(1S,4S,7Z,10S,16E,21R)-7-ethylidene-、罗咪酯肽、罗米地辛

产品性质

CAS编号：128517-07-7

分子式：C24H36N4O6S2

分子量：540.7

MDL号：MFCD18433404

PubChem编号：5352062

别名：罗咪酯肽|罗米地辛

英文别名：Romidepsin|Istodax|Depsipeptide|Chromadax|FK228|128517-07-7|Antibiotic FR 901228|FR901228|FK 228|FK-228|FR 901228|NSC-630176|FR-901228|romidepsina|romidepsine|romidepsinum|NSC 630176|CHEBI61080|CX3T89XQBK|CHEMBL343448|(1S,4S,7Z,10S,16E,21R)-7-ethylidene-

规格或纯度：≥98%

英文名称：Romidepsin (FK228, Depsipeptide)

生化机理：Romidepsin, a selective inhibitor of histone deacetylases (HDACs), was approved for the treatment of cutaneous T-cell lymphoma in November 2009 by the U.S. FDA. Romidepsin is a member of a new class of antineoplastic agents active in T-cell lymphoma, the histone deacetylase inhibitors. Romidepsin strongly down-regulated expression of the immunosuppressive cytokine, interleukin (IL)-10, frequently overexpressed in CTCL, at both the RNA and protein level in CTCL cell lines and at the RNA level in primary CTCL cells. Romidepsin also increased expression of IFNG RNA and decreased expression of IL-2 and IL-4 RNA, althoμgh to a lesser extent compared to IL-10. Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively. Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. Romidepsin promotes apoptosis in chronic lymphocytic leukemia (CLL) cells at a concentration corresponding to that at which H3 and H4 acetylation and HDAC inhibition occurs, selectively involving activation of caspase 8 and effector caspase 3, as well as down-regulation of c-FLIP protein.Potent HDAC1 and HDAC2 inhibitor (IC 50 values are 36 and 47 nM at HDAC1 and HDAC2 respectively). Induces apoptosis, cell-cycle arrest and modulates cytokine expression in cancer cells. Antitumor agent. Active in vivo and in vitro .

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，这些产品最多可以使用一周。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：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)。Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s 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.

ALogP：2.2

IUPAC Name：(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

INCHI：InChI=1S/C24H36N4O6S2/c1-6-16-21(30)28-20(14(4)5)24(33)34-15-9-7-8-10-35-36-12-17(22(31)25-16)26-23(32)19(13(2)3)27-18(29)11-15/h6-7,9,13-15,17,19-20H,8,10-12H2,1-5H3,(H,25,31)(H,26,32)(H,27,29)(H,28,30)/b9-7+,16-6-/t15-,17-,19-,20+/m1/s1

InChi Key：OHRURASPPZQGQM-GCCNXGTGSA-N

Canonical SMILES：CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

Isomeric SMILES：C/C=C\1/C(=O)N[C@H](C(=O)O[C@H]\2CC(=O)N[C@@H](C(=O)N[C@H](CSSCC/C=C2)C(=O)N1)C(C)C)C(C)C

RTECS：YV9399000

PubChem CID：5352062

CAS Registry No.：128517-07-7

ChEMBL Ligand：CHEMBL343448

Wikipedia：Romidepsin

PEP：romidepsin

Reactome Reaction：R-HSA-9679787

Reactome Drug：R-ALL-9679799

DrugCentral Ligand：4119

溶解性：DMSO 10 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

象形图：

信号词：Danger

危险声明：H301 Toxic if swallowedH341 Suspected of causing genetic defectsH317 May cause an allergic skin reactionH400 Very toxic to aquatic lifeH410 Very toxic to aquatic life with long lasting effects

预防措施声明：P261,P273,P280,P302+P352,P321,P405,P501,P264,P281,P270,P272,P333+P313,P362+P364,P391,P330,P203,P301+P316,P318

产品包装