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    YM155 (Sepantronium Bromide)
    YM155 (Sepantronium Bromide)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0771
    CAS #: 781661-94-7Purity ≥98%

    Description: YM155 (also called Sepantronium Bromide; YM-155; YM 155) is a novel and potent survivin inhibitor with potential anticancer activity. It inhibits survivin promoter activity with an IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; it is a small-molecule proapoptotic agent that does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 exhibits a potent suppressive activity against survivin but has little effect on expression levels of other IAP family members or B-cell lymphoma 2 (BCL-2) related proteins. 

    References:  BMC Cancer. 2012 Dec 26;12:619. 

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    Molecular Weight (MW)443.29
    FormulaC20H19BrN4O3
    CAS No.781661-94-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 55 mg/mL (124.07 mM) 
    Water: 89 mg/mL (200.8 mM)
    Ethanol: 6 mg/mL (13.53 mM)
    Solubility (In vivo)Saline: 30 mg/mL
    Other info

    YM-155; Sepantronium bromide; YM155; YM 155; 

    1-(2-methoxyethyl)-2-methyl-3-(pyrazin-2-ylmethyl)benzo[f]benzimidazol-3-ium-4,9-dione;bromide; 

    Chemical Name: 3-(2-methoxyethyl)-2-methyl-4,9-dioxo-1-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide.

    SMILES Code: O=C(C1=C2[N+](CCOC)=C(C)N1CC3=NC=CN=C3)C4=C(C=CC=C4)C2=O.[Br-]           


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    In Vitro

    Kinase Assay: Promoter-luciferase reporter assay; A 2,767-bp sequence of human survivin gene promoter is isolated from human genomic DNA by PCR using Pyrobest polymerase and the following primers: 5'-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3' and 5'-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3'. The resulting PCR fragment is digested with XhoI/HindIII and ligated into the XhoI/HindIII cleavage site of the pGL3-Basic vector. The resulting plasmid is named pSUR-luc. DNA sequencing is done on all amplified sequences by a DNA sequencer. The activity of pSUR-luc is confirmed by luciferase assay with transiently transfected HeLa-S3 cells. Luciferase assay is done. The pGL3 control vector, which contains the SV40 promoter and enhancer sequences, is used. HeLa cells are stably transfected with pSUR-luc and pSV2bsr by Lipofect-AMINE 2000. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named HeLa-SURP-luc. CHO cells are stably transfected with pGL3-control and pSV2bsr. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named CHO-SV40-luc. Stocked cells from the HeLa-SURP-luc and CHO-SV40-luc clones are used for chemical screening and characterization of YM155. YM155 in DMSO are added to the cells, which had been seeded the previous day on 96-well plastic plates at 5 × 103 per well. Luciferase activity is measured 24 hours later. IC50 is calculated by logistic analysis.


    Cell Assay: Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375); 100nM; 40 hrs; Cells are seeded in 96-well plates at a density of 5-40 × 103. YM155 is dissolved in DMSO and added to cells for 48 hours. Then the cell count is determined by sulforhodamine B assay. 

    YM155 is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. YM155 significantly inhibits endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 through transcriptional inhibition of the survivin gene promoter. On the contrary YM155 shows no sufficient effect on protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at 100 nM. YM155 indicates great apoptosis in human cancer cell lines including PC-3 and PPC-1 with a concomitant increase in caspase-3 activity. YM155 potently inhibits human cancer cell lines (mutated or truncated p53) including PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50 from 2.3 to 11 nM, respectively. YM155 increases the sensitivity of NSCLC cells to γ-radiation. The combination of YM155 and γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA.

    In VivoYM155 completely inhibits the tumor growth of PC-3 s.c. xenografted prostate tumors at doses of 3 and 10 mg/kg, without body weight loss and blood cell count decrease. Pharmacokinetic analysis shows that YM155 is highly distributed to tumor tissue. Moreover, YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. The combination therapy with YM155 and γ-radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice
    Animal model PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu) 
    Formulation & Dosage Saline;  5 mg/kg; Subcutaneous injection by an implanted micro-osmotic pump
    References

    Cancer Res. 2007 Sep 1;67(17):8014-21;  Clin Cancer Res, 2008, 14(20), 6496-6504.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    YM155 (Sepantronium Bromide)

     

    YM155 (Sepantronium Bromide)

     

    YM155 (Sepantronium Bromide)


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