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Sepantronium bromide

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Chemical Structure| 781661-94-7 同义名 : -
CAS号 : 781661-94-7
货号 : A307284
分子式 : C20H19BrN4O3
纯度 : 98%
分子量 : 443.294
MDL号 : MFCD11983133
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(112.79 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(112.79 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Survivin

    Survivin, IC50:0.54 nM
描述 Survivin is a member of the inhibitor of apoptosis (IAP) protein family and has been implicated in both cell survival and regulation of mitosis in cancer. YM155 is a potent survivin inhibitor with IC50 value of 0.54 nM for survivin promoter activity[2]. YM155 suppressed expression of survivin and induced apoptosis in PC-3 and PPC-1 human hormone-refractory prostate cancer (HRPC) cell lines at 10 nM, but showed little effect on expression levels of other IAP- or Bcl-2-related proteins up to 100 nM. In a s.c. xenografted PC-3 tumor model in mice, 3-day continuous infusions of YM155 at 3 to 10 mg/kg induced massive tumor regression accompanied by suppression of intratumoral surviving and no significant decreases in body weight were observed[2]. Glioma cell lines responded in a dose and time-dependent manner to YM-155 with reduction of cell numbers. U373, LN18, LNZ428, T98G, LN229, and LNZ308 cells exhibited an IC50 of ~ 10-75 nM, while A172 cells were resistant to YM-155 with IC50 ~ 250 nM[3]. Exposure of U373 and LN18 (YM-155 sensitive) glioma cells to 25 nM of YM-155 for 24 h caused a marked loss of mitochondrial membrane potential compared with the control group[3]. Primary effusion lymphoma-patient-derived xenograft mice were treated with YM-155 (5 mg/kg) from days 2-22. The volume of ascites was significantly less in YM155-treated mice than in control mice on day 22 (0.75 mL [median, range 0-2.56 mL] vs. 3.96 mL [median, range 0.7-5.29 mL], p < 0.01)[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780cis 0-100 nM Function Assay 24 h induces Survivin downregulation  24262875
A2780cis 5-100 nM Apoptosis Assay 24/48 h increases apoptosis in a concentration-dependent manner 24262875
A2780p 0-100 nM Function Assay 24 h induces Survivin downregulation  24262875
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.28mL

2.26mL

1.13mL

22.56mL

4.51mL

2.26mL
参考文献

[2]Nakahara T, Kita A, Yamanaka K, Mori M, Amino N, Takeuchi M, Tominaga F, Hatakeyama S, Kinoyama I, Matsuhisa A, Kudoh M, Sasamata M. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts. Cancer Res. 2007 Sep 1;67(17):8014-21. doi: 10.1158/0008-5472.CAN-07-1343. Erratum in: Cancer Res. 2012 Aug 1;72(15):3886. Mori, Masamichi [added]; Amino, Nobuaki [added]; Hatakeyama, Shinji [added];Minematsu, Tsuyoshi [removed]; Shirasuna, Kenna[removed]. PMID: 17804712.

[3]Jane EP, Premkumar DR, DiDomenico JD, Hu B, Cheng SY, Pollack IF. YM-155 potentiates the effect of ABT-737 in malignant human glioma cells via survivin and Mcl-1 downregulation in an EGFR-dependent context. Mol Cancer Ther. 2013 Mar;12(3):326-38. doi: 10.1158/1535-7163.MCT-12-0901. Epub 2013 Jan 16. PMID: 23325792; PMCID: PMC3596447.

[4]Kojima Y, Hayakawa F, Morishita T, Sugimoto K, Minamikawa Y, Iwase M, Yamamoto H, Hirano D, Imoto N, Shimada K, Okada S, Kiyoi H. YM155 induces apoptosis through proteasome-dependent degradation of MCL-1 in primary effusion lymphoma. Pharmacol Res. 2017 Jun;120:242-251. doi: 10.1016/j.phrs.2017.04.006. Epub 2017 Apr 8. PMID: 28396094.