YM155
(Synonyms: 4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-D]咪唑溴化物,Sepantronium bromide,YM-155) 目录号 : GC13107
YM155是一种基于imidazolium的小分子化合物，能有效抑制survivin启动子活性，IC50值为0.54nM。
Cas No.:781661-94-7
Sample solution is provided at 25 µL, 10mM.
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YM155, a small imidazolium-based compound, potently inhibits survivin promoter activity with an IC50 value of 0.54nM [1]. YM155 can suppress survivin expression through the disruption of SP1 binding to the survivin core promoter and of ILF3–p54/nrb complex[2]. YM155 has been widely used to induce tumor cell apoptosis and promote tumor regression in diverse cell and animal models[3].
In vitro, YM155 treatment for 120 hours significantly inhibited the proliferation of UKF-NB-3 and UKF-NB-6 cells with IC50 values of 0.49 and 0.65nM, respectively[4]. Treatment of H1299 cells with YM155 at 40nM for 24h significantly induced cell death and promoted mitochondrial dysfunction, leading to a reduction in tricarboxylic acid (TCA) cycle intermediates[5]. Treatment with 10nM YM155 for 24 hours significantly inhibited PANC-1 cell viability and induced downregulation of PI3K, p-ERK, and p-STAT3 in PANC-1 cells[6].
In vivo, YM155 treatment via subcutaneous injection at a dose of 2 mg/kg/day for 21 days remarkably reduced tumor growth in the SH-SY5Y cell xenograft model of mice, without affecting body weight[7]. Continuous subcutaneous infusion of YM155 (5mg/kg/day) for 21 days significantly inhibited the development of ascites in Primary effusion lymphoma (PEL) xenograft mice[8].
References:
[1] Nakahara T, Takeuchi M, Kinoyama I, et al. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts[J]. Cancer research, 2007, 67(17): 8014-8021.
[2] Rauch A, Hennig D, Schäfer C, et al. Survivin and YM155: how faithful is the liaison?[J]. Biochimica et Biophysica Acta (BBA)-Reviews on Cancer, 2014, 1845(2): 202-220.
[3] Tolcher A W, Quinn D I, Ferrari A, et al. A phase II study of YM155, a novel small-molecule suppressor of survivin, in castration-resistant taxane-pretreated prostate cancer[J]. Annals of oncology, 2012, 23(4): 968-973.
[4] Voges Y, Michaelis M, Rothweiler F, et al. Effects of YM155 on survivin levels and viability in neuroblastoma cells with acquired drug resistance[J]. Cell death & disease, 2016, 7(10): e2410-e2410.
[5] Mondal A, Jia D, Bhatt V, et al. Ym155 localizes to the mitochondria leading to mitochondria dysfunction and activation of AMPK that inhibits BMP signaling in lung cancer cells[J]. Scientific reports, 2022, 12(1): 13135.
[6] Na Y S, Yang S J, Kim S M, et al. YM155 induces EGFR suppression in pancreatic cancer cells[J]. PloS one, 2012, 7(6): e38625.
[7] Li X, Yang F, He N, et al. YM155 inhibits neuroblastoma growth through degradation of MYCN: A new role as a USP7 inhibitor[J]. European Journal of Pharmaceutical Sciences, 2023, 181: 106343.
[8] Kojima Y, Hayakawa F, Morishita T, et al. YM155 induces apoptosis through proteasome-dependent degradation of MCL-1 in primary effusion lymphoma[J]. Pharmacological research, 2017, 120: 242-251.
YM155是一种基于imidazolium的小分子化合物，能有效抑制survivin启动子活性，IC50值为0.54nM[1]。YM155通过破坏SP1与survivin核心启动子的结合，以及干扰ILF3-p54/nrb复合物的形成，从而抑制survivin的表达[2]。YM155已广泛应用于多种细胞和动物模型中，用于诱导肿瘤细胞凋亡并促进肿瘤消退[3]。
在体外，YM155处理120小时可显著抑制UKF-NB-3和UKF-NB-6细胞的增殖，IC50值分别为0.49nM和0.65nM[4]。使用40nM YM155处理H1299细胞24小时，能显著诱导细胞死亡并促进线粒体功能障碍，导致三羧酸(TCA)循环中间产物减少[5]。用10nM的YM155处理PANC-1细胞24小时，可显著抑制细胞活力，并下调PI3K、p-ERK和p-STAT3的表达[6]。
在体内，每日皮下注射2 mg/kg/day剂量的YM155连续21天，能显著抑制SH-SY5Y细胞移植瘤小鼠的肿瘤生长，且不影响体重[7]。持续皮下输注YM155（5 mg/kg/day）21天，可显著抑制原发性渗出性淋巴瘤移植瘤小鼠腹水的形成[8]。
| Cell experiment [1]: | |
Cell lines | PC-3 cells |
Preparation Method | PC-3 cells were cultured in DMEM medium supplemented with 10% heat-inactivated fetal bovine serum and placed in a 37°C humidified incubator at 5% CO2. After 48h of culture in the presence of YM155 (1, 10, 100, and 1000nM), PC-3 cells were harvested by trypsin digestion and centrifugation and resuspended in DMEM medium. The cell suspension was diluted in an equal volume of trypan blue (0.4% working solution). Live (unstained) and dead (stained) cells were counted using a blood cell counter. |
Reaction Conditions | 1, 10, 100, and 1000nM; 48h |
Applications | YM155 significantly inhibited the viability of PC-3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c-nu mice |
Preparation Method | Six-week-old female BALB/c-nu mice were maintained in a standard sterile environment. SH-SY5Y cells (2×106) were collected and mixed with an equal volume of Matrigel and injected subcutaneously into the flank of mice. After tumor formation, mice were randomly divided into two groups: vehicle group (saline) or YM155 group. YM155 was injected subcutaneously continuously at a dose of 2mg/kg/day for 21 days using a micro-osmotic pump. Tumor diameter was measured twice a week, and tumor volume was calculated as the product of length × width2×0.5. |
Dosage form | 2mg/kg/day for 21 days; s.c. |
Applications | YM155 treatment remarkably reduced tumor growth in the SH-SY5Y cell xenograft model of mice. |
References: | |
| Cas No. | 781661-94-7 | SDF | |
| 别名 | 4,9-二氢-1-(2-甲氧基乙基)-2-甲基-4,9-二氧代-3-(2-吡嗪甲基)-1H-萘并[2,3-D]咪唑溴化物,Sepantronium bromide,YM-155 | ||
| 化学名 | 1-(2-methoxyethyl)-2-methyl-3-(pyrazin-2-ylmethyl)benzo[f]benzimidazol-3-ium-4,9-dione;bromide | ||
| Canonical SMILES | CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-] | ||
| 分子式 | C20H19BrN4O3 | 分子量 | 443.3 |
| 溶解度 | ≥ 22.15 mg/mL in DMSO, ≥ 13.49 mg/mL in EtOH with ultrasonic, ≥ 96.2 mg/mL in Water with ultrasonic | 储存条件 | Store at -20°C |
| 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 | 2.2558 mL | 11.279 mL | 22.5581 mL |
| 5 mM | 451.2 μL | 2.2558 mL | 4.5116 mL |
| 10 mM | 225.6 μL | 1.1279 mL | 2.2558 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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