YM155 (Survivin抑制剂)

YM155 (Survivin抑制剂)

YM155

产品规格: 5mg    10mg    1ml (10mM/DMSO) 

CAS: 781661-94-7

保存条件: Store at -20℃ for 3 year(Powder); In DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

产品介绍:

基本信息：

CAS：781661-94-7

分子式：C20H19BrN4O3

分子量：443.29

纯度：≥98%

溶解性：可溶于水（>89mg/ml）、二甲基亚砜（>89mg/ml）、乙醇（>24mg/ml）、二甲基甲酰胺（~3mg/ml）和多溴联苯（pH7.2）（~10mg/ml）。

作用靶点：Survivin; Autophagy;

作用通路：Apoptosis; Autophagy;

用途/描述：YM155 (Sepantronium Bromide) 是一种有效的 survivin 抑制药，通过抑制 Survivin 启动子活性而发挥作用，在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM；对SV40启动子活性抑制作用不显著，能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivin 和 XIAP、调节自噬并诱导自噬依赖的DNA损伤。

体外研究：

Sepantronium bromide (YM155; 30 μM) is not sensitive to survivn gene promoter-driven luciferase reporter activity. Sepantronium bromide shows significant supression on endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 via transcriptional inhibition of the survivin gene promoter. Sepantronium bromide (100 nM) does not affect protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin. Sepantronium bromide potently inhibits human cancer cell lines (mutated or truncated p53) such as PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50s ranging from 2.3 to 11 nM, respectively.

Sepantronium bromide resultin in an increase in sensitivity of NSCLC cells to γ-radiation. Sepantronium bromide combined with γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. In addition, Sepantronium bromide delays the repair of radiation-induced double-strand breaks in nuclear DNA.

体内研究：

Sepantronium bromide (YM155; 3 and 10 mg/kg) inhibits the tumor growth in PC-3 xenografts, without obvious body weight loss and blood cell count decrease. Sepantronium bromide is highly distributed to tumor tissue in vivo. Sepantronium bromide shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. Sepantronium bromide in combination with γ-radiation shows potent antitumor activity against H460 or Calu6 xenografts in nude mice.

In this orthotopic renal and metastatic lung tumors models, Sepantronium bromide and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images.

特别提示：本公司的所有产品仅可用于科研实验，严禁用于临床医疗及其他非科研用途！