2. Apoptosis Autophagy
  3. Survivin Autophagy
  4. Sepantronium hydrochloride

Sepantronium hydrochloride  (Synonyms: YM-155 hydrochloride)

目录号: HY-10194A
产品使用指南

摩尔计算器

Sepantronium hydrochloride (YM-155 hydrochloride) 是一种新型 survivin 抑制剂，对 survivin 启动子的 IC50 为 0.54 nM。

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Sepantronium hydrochloride Chemical Structure

Sepantronium hydrochloride Chemical Structure

CAS No. : 355406-09-6

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Sepantronium hydrochloride 的其他形式现货产品:

Other Forms of Sepantronium hydrochloride:

Sepantronium hydrochloride 相关抗体

Top Publications Citing Use of Products

    Sepantronium hydrochloride purchased from MCE. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617.   [Abstract]

    A2780 CSLCs are treated in the presence or absence of AS602801 (7.5 μM) and/or YM155 (10 nM) for 3 days, and then subjected to western blot analysis of survivin and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

    Sepantronium hydrochloride purchased from MCE. Usage Cited in: Nutrients. 2018 Mar 15;10(3). pii: E353.  [Abstract]

    Influences of YM155, a chemical inhibitor of survivin on ABT-737-induced apoptosis are analyzed by western blot.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Sepantronium hydrochloride (YM-155 hydrochloride) is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity[1].

    IC50 & Target

    IC50: 0.54 nM (survivin)
    体外研究
    (In Vitro)

    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[1].
    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[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Sepantronium hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    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[1].
    Sepantronium bromide (YM155) in combination with γ-radiation shows potent antitumor activity against H460 or Calu6 xenografts in nude mice[2].
    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[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    398.84

    Formula

    C20H19ClN4O3
    CAS 号
    性状

    固体

    颜色

    Light brown to brown

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    纯度 & 产品资料
    参考文献
    Cell Assay
    [1]

    The antiproliferative activity of Sepantronium bromide is measured. After treatment with Sepantronium bromide for 48 h, the cell count is determined by sulforhodamine B assay. The GI50 value is calculated by logistic analysis, which is the drug concentration resulting in a 50% reduction in the net protein increase (as measured by sulforhodamine B staining) in control cells during the drug incubation. The assay is done in triplicate, and the mean GI50 value is obtained from the results of four independent assays.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Five-week-old male nude mice (BALB/c nu/nu) are used for the assay. PC-3 cells (2×106-3×106) are injected into the flanks of the mice and allowed to reach a tumor volume of > 100 mm3 in tumor volume (length×width2×0.5). Sepantronium bromide is s.c. administered as a 3-day continuous infusion per week for 2 weeks using an implanted micro-osmotic pump or i.v. administered five times a week for 2 weeks. The percentage of tumor growth inhibition 14 days after initial Sepantronium bromide administration is calculated for each group using the following formula: MTV=100×{1-[(MTV of the treated group on day 14)-(MTV of the treated group on day 0)]/[(MTV of the control group on day 14)-(MTV of the control group on day 0)]}, where MTV is mean tumor volume. For both the frozen tumors and plasma samples, survivin expression levels are analyzed by Western blotting and Sepantronium bromide concentration by high-performance liquid chromatography/triple quadrupole mass spectrometry (LC/MS/MS) using validated methods.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Sepantronium hydrochloride 相关分类

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    • 稀释计算器

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sepantronium355406-09-6YM-155YM155YM 155SurvivinAutophagyInhibitorinhibitorinhibit

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