YM155 (Synonyms: Sepantronium bromide) |
| Catalog No.GC13107 |
A small molecule survivin suppressant
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 781661-94-7
Sample solution is provided at 25 µL, 10mM.
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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
| 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. | |
| Cas No. | 781661-94-7 | SDF | |
| Synonyms | Sepantronium bromide | ||
| Chemical Name | 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-] | ||
| Formula | C20H19BrN4O3 | M.Wt | 443.3 |
| Solubility | ≥ 22.15 mg/mL in DMSO, ≥ 13.49 mg/mL in EtOH with ultrasonic, ≥ 96.2 mg/mL in Water with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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