Romidepsin (FK228, depsipeptide)
(Synonyms: 罗米地辛; FK 228; FR 901228; NSC 630176) 目录号 : GC11334
Romidepsin (FK228, depsipeptide)是一种有效且选择性的组蛋白去乙酰化酶（HDAC）抑制剂，抑制HDAC1，HDAC2，HDAC4和HDAC6的IC50值分别为36nM，47nM，510nM和1.4μM。
Cas No.:128517-07-7
Sample solution is provided at 25 µL, 10mM.
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Romidepsin (FK228, depsipeptide) is an effective and selective histone deacetylase (HDAC) inhibitor, with IC50 values of 36nM, 47nM, 510nM, and 1.4μM for HDAC1, HDAC2, HDAC4, and HDAC6, respectively [1-2]. HDAC is a type of epigenetic regulator, and the HDAC1 is expressed in many tumor types [3]. Romidepsin has anti-tumor activity and can induce cell cycle arrest, cell differentiation, apoptosis, and gene expression changes in malignant tumor cells [4].
In vitro, Romidepsin (0.5-30ng/mL; 72h) treatment can dose-dependently reduce the cell viability of neuroblastoma cell lines (NB), and the cell morphology shows a round, denser, and non-adherent state. In different NB cell lines, the IC50 range of Romidepsin is 1-6.5ng/mL [5]. Romidepsin (0-60nM; 0-48h) can induce G2/M phase cell cycle arrest in HCC cells in a time- and dose-dependent manner and promote cell apoptosis, increasing the expression of c-caspase-3, c-caspase-9, and c-PARP proteins [6].
In vivo, Romidepsin (1-1.7mg/kg/day; injected once every 3 or 4 days, for a total of five times; i.p.) significantly inhibits the growth of xenograft mouse KCNR tumors. Within 6 hours of a single dose, the p21 level in the mouse tumors increased nearly 7 times compared to the control group, and reached 25 times at 24 hours [5]. Romidepsin (0.5 and 1mg/kg/day; once every 3 days, for 21 days; i.p.) significantly inhibits tumor growth in Huh7 tumor-bearing mice and increases the expression of p-cdc25C, ki67, c-caspase-3, and c-PARP, and reduces the expression of Ki-67 [6].
References:
[1] Karen M VanderMolen, William McCulloch, Cedric J Pearce and Nicholas H Oberlies. Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma. The Journal of Antibiotics 2011: 64, 525-531
[2] Furumai R, Matsuyama A, Kobashi N, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002;62(17):4916-4921.
[3] Pojani E, Barlocco D. Romidepsin (FK228), A Histone Deacetylase Inhibitor and its Analogues in Cancer Chemotherapy. Curr Med Chem. 2021;28(7):1290-1303.
[4] Jyoti Panicker, Zhijie Li, Christine McMahon, et al. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells. Cell Cycle 2010 9:9, 1830-1838.
[5] Panicker J, Li Z, McMahon C, et al. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells. Cell Cycle. 2010;9(9):1830-1838.
[6] Sun WJ, Huang H, He B, 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;127:90-100.
Romidepsin (FK228, depsipeptide)是一种有效且选择性的组蛋白去乙酰化酶（HDAC）抑制剂，抑制HDAC1，HDAC2，HDAC4和HDAC6的IC50值分别为36nM，47nM，510nM和1.4μM [1-2]。HDAC是一类表观遗传调节因子，HDAC1在许多肿瘤类型中表达 [3]。Romidepsin具有抗肿瘤活性，能诱导恶性肿瘤中的细胞周期停滞、细胞分化、凋亡和基因表达改变 [4]。
在体外，Romidepsin（0.5–30ng/mL; 72h）处理能够剂量依赖性降低神经母细胞瘤细胞系（NB）的细胞活力，并且细胞形态表现为圆形、更密集且不贴壁的状态。在不同的NB细胞系中，Romidepsin的IC50范围为1-6.5ng/mL [5]。Romidepsin（0-60nM; 0-48h）能够以时间和剂量依赖性方式诱导HCC细胞中G2/M期细胞周期停滞，并促进细胞凋亡，增加了细胞中c-caspase-3、c-caspase-9和c-PARP蛋白的表达 [6]。
在体内，Romidepsin（1-1.7mg/kg/day; 每3或4天注射一次，共五次; i.p.）显著抑制异种移植小鼠KCNR肿瘤的生长。单剂量给药6小时内，小鼠肿瘤中的p21水平与对照组相比增加了近7倍，并在24小时达到25倍 [5]。Romidepsin（0.5和1mg/kg/day; 每3天一次, 21天; i.p.）显著抑制Huh7荷瘤小鼠的肿瘤生长，并升高了肿瘤中p-cdc25C、ki67、c-caspase-3和c-PARP的表达，以及降低Ki-67的表达 [6]。
| Cell experiment [1]: | |
Cell lines | Human Neuroblastoma (NB) Cell Lines |
Preparation Method | NB cells (5,000 to 10,000 cells/well) were seeded into 96 flat-bottomed well plates, and six replicate wells were incubated with different concentrations of Romidepsin for 72h. In some experiments, cell growth was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay or an MTS/PMS colorimetric assay after 72h of Romidepsin treatment, as previously described. Samples were assessed according to manufacturer’s recommendations. The inhibition of viability was represented as a percentage of control cells. Each experiment was repeated 2–3 times and variability among the experiments on the same cell line and between MTT and MTS was less than 10%. |
Reaction Conditions | 0.5–30ng/mL; 72h |
Applications | Romidepsin dose-dependently reduced the cell viability of the NB cell lines, and the cell morphology underwent extensive changes, presenting as round, more dense and non-adherent states. In different NB cell lines, the IC50 range of Romidepsin was 1-6.5ng/mL. |
| Animal experiment [1]: | |
Animal models | Nude mice (Subcutaneous NB xenograft model) |
Preparation Method | Two million KCNR NB tumor cells were injected subcutaneous into the right backside of nude mice. Tumor size was measured with calipers. Tumor volume (V) was calculated as follows: V = a2 × b/4, where a is the width (small diameter) and b the length (large diameter) of the tumor in millimeters. When the tumor size reached 200mm3, mice received intraperitoneal injections of vehicle control, 1.0, or 1.7mg/kg Romidepsin every 3 or 4 days for a total of 5 doses. To assess in treatment related changes in tumor gene expression, mice were given a single dose of romidepsin (1.7mg/kg) and tumors were harvested at 6 or 24h. |
Dosage form | 1-1.7mg/kg/day; every 3 or 4 days, five times; i.p. |
Applications | Romidepsin significantly inhibited the growth of KCNR tumors in xenograft mice. |
References: | |
| Cas No. | 128517-07-7 | SDF | |
| 别名 | 罗米地辛; FK 228; FR 901228; NSC 630176 | ||
| 化学名 | (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 | ||
| 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 | ||
| 分子式 | C24H36N4O6S2 | 分子量 | 540.7 |
| 溶解度 | ≥ 27.035mg/mL in DMSO, ≥ 35.27 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C,unstable in solution, ready to use. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8495 mL | 9.2473 mL | 18.4945 mL |
| 5 mM | 0.3699 mL | 1.8495 mL | 3.6989 mL |
| 10 mM | 0.1849 mL | 0.9247 mL | 1.8495 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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