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
A small molecule survivin suppressant
Cas No.:781661-94-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
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Cell lines |
PC-3 and PPC-1 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1 μM, 48 hours |
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Applications |
In both cell lines, YM155, at concentrations from 10 to 1000 nM, significantly decreased the viability of cells in a dose-dependent manner. When exposed to YM155, PC-3 and PPC-1 showed a concomitant increase in caspase-3 activity. These results suggest that YM155 induces apoptosis in human HRPC cells. |
| Animal experiment: [1] | |
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Animal models |
BALB/c nu/nu mice injected with PC-3 cells |
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Dosage form |
Subcutaneous injection, 10 mg/kg |
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Applications |
Mice with large established s.c. xenografted PC-3 tumors received a 3-day continuous infusion of YM155 at 10 mg/kg. Saline control animals showed rapid tumor growth from day 0 (366 mm3) to day 7 (1,123 mm3), with no change in intratumoral surviving and actin protein levels. In contrast, animals treated with YM155 showed tumor regression from day 0 (292 mm3) to day7 (162 mm3), and a clear decrease in intratumoral survivin levels on days 3 and 7 was observed. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. Cancer research, 2007, 67(17): 8014-8021. | |
Sepantronium bromide, also known as YM155, is a novel small-molecule suppressant of surviving, the smallest member of inhibitor of apoptosis (IAP) gene family. It exhibits a potent suppressive activity against survivin but has little effect on expression levels of other IAP family members or B-cell lymphoma 2 (BCL-2) related proteins. YM155 also suppresses proliferation in a broad range of human cancer cell lines, induces tumor regression in non-small cell lung cancer (NSCLC), melanoma, bladder, aggressive non-Hodgkin lymphoma, and breast cancer xenograft models, reduces spontaneous metastases, and significantly prolongs the survival of animal harboring established metastatic tumors derived from a human triple-negative breast cancer (TNBC) cell lines.
Reference
[1].Naoki Kaneko, Kentaro Yamanaka, Aya Kita, Kenji Tabata, Takafumi Akabane, and Masamichi Mori. Synergistic antitumor activities of sepantronium bromide (YM155), a surviving suppressant, in combination with microtubule-targeting agents in triple-negative breast cancer cells. Biol Pharm Bull 2013.
[2].Yan-Fang Tao, Jun Lu, Xiao-Juan Du, Li-Chao Sun, Xuan Zhao, Liang Peng, Lan Cao, Pei-Fang Xiao, Li Pang, Dong Wu, Na Wang, Xing Feng, Yan-Hong Li, Jian Ni, Jian Wang and Jian Pan. Survivin selective inhibitor YM155 induce apoptosis in SK-NEP-1 Wilms tumor cells. BMC Cancer 2012, 12:619
| 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 | 0.4512 mL | 2.2558 mL | 4.5116 mL |
| 10 mM | 0.2256 mL | 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。