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

Sepantronium hydrochloride  (Synonyms: YM-155 hydrochloride)

Cat. No.: HY-10194A
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Sepantronium hydrochloride (YM-155 hydrochloride) is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.

For research use only. We do not sell to patients.

Sepantronium hydrochloride Chemical Structure

Sepantronium hydrochloride Chemical Structure

CAS No. : 355406-09-6

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Sepantronium hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Sepantronium hydrochloride purchased from MedChemExpress. 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 MedChemExpress. 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.

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    Description

    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)
    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].

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

    Sepantronium hydrochloride Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    398.84

    Formula

    C20H19ClN4O3
    CAS No.
    Appearance

    Solid

    Color

    Light brown to brown

    SMILES

    O=C(C1=C2[N+](CC3=NC=CN=C3)=C(C)N1CCOC)C4=C(C=CC=C4)C2=O.[Cl-]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, sealed storage, away from moisture

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

    Purity & Documentation
    References
    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.
    References
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    Sepantronium hydrochloride Related Classifications

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    Help & FAQs
    • 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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