1. Apoptosis
    Autophagy
  2. Survivin
    Autophagy
  3. Sepantronium bromide

Sepantronium bromide (Synonyms: YM-155)

Cat. No.: HY-10194 Purity: ≥98.0%
Handling Instructions

YM-155 (Sepantronium bromide) est un inhibiteur de survivine avec un IC50 de 0,54 nM.

Sepantronium bromide (YM-155) is a survivin inhibitor with an IC50 of 0.54 nM.

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

Sepantronium bromide Chemical Structure

Sepantronium bromide Chemical Structure

CAS No. : 781661-94-7

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 84 In-stock
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50 mg USD 348 In-stock
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100 mg USD 492 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Sepantronium bromide:

Top Publications Citing Use of Products

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

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

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

    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).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sepantronium bromide (YM-155) is a survivin inhibitor with an IC50 of 0.54 nM[1].

    IC50 & Target

    IC50: 0.54 nM (Survivin)[1]

    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.

    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
    Molecular Weight

    443.29

    Formula

    C₂₀H₁₉BrN₄O₃

    CAS No.
    SMILES

    O=C1C2=C(C(C3=CC=CC=C31)=O)[N+](CC4=NC=CN=C4)=C(C)N2CCOC.[Br-]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (225.59 mM; Need ultrasonic)

    DMSO : 50 mg/mL (112.79 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2559 mL 11.2793 mL 22.5586 mL
    5 mM 0.4512 mL 2.2559 mL 4.5117 mL
    10 mM 0.2256 mL 1.1279 mL 2.2559 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2 mg/mL (4.51 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: 2 mg/mL (4.51 mM); Clear solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (112.79 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    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

    Purity: 98.91%

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    Keywords:

    SepantroniumYM-155YM155YM 155SurvivinAutophagyInhibitorinhibitorinhibit

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    Product Name:
    Sepantronium bromide
    Cat. No.:
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