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Sepantronium Bromide

Sepantronium Bromide YM-155

Sepantronium Bromide(YM155)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。Phase 2。

货号：
TK0127
规格：

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	781661-94-7
生物活性	Sepantronium bromide (YM-155) is a survivin inhibitor with an IC50 of 0.54 nM.
分子式	C20H19BrN4O3
分子量	443.29
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	H2O : 100 mg/mL (225.59 mM; Need ultrasonic) DMSO : 50 mg/mL (112.79 mM; Need ultrasonic)
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 (YM155) 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 (YM-155) and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images.
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 (YM155) 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.
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纯度及产品资料	≥98%

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