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YM155
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YM155图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
100mg电议

产品介绍
YM155 (YM-155) 是一种存活素抑制剂,IC50 为 0.54 nM。

Cell lines

PC-3 and PPC-1 cells

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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1 μM, 48 hours

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 models

BALB/c nu/nu mice injected with PC-3 cells

Dosage form

Subcutaneous injection, 10 mg/kg

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.

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.

产品描述

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