YM-155 hydrochloride

CAS No. 355406-09-6

YM-155 hydrochloride( YM155 hydrochloride | YM 155 hydrochloride )

Catalog No. M14215 CAS No. 355406-09-6

A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    YM-155 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.
  • Description
    A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM; does not significantly inhibit SV40 promoter activity (>30 uM); suppresses expression of survivin and induces apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nM, without effect on IAP- or Bcl-2-related proteins; induces massive tumor regression in PC-3 tumor mice model (3-10 mg/kg).Blood Cancer Phase 1 Discontinued.
  • 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. 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.
  • 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. 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.
  • Synonyms
    YM155 hydrochloride | YM 155 hydrochloride
  • Pathway
    Apoptosis
  • Target
    IAP
  • Recptor
    IAP
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    355406-09-6
  • Formula Weight
    398.8429
  • Molecular Formula
    C20H19ClN4O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Cl-]
  • Chemical Name
    1H-Naphth[2,3-d]imidazolium, 4,9-dihydro-3-(2-methoxyethyl)-2-methyl-4,9-dioxo-1-(2-pyrazinylmethyl)-, chloride (1:1)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Nakahara T, et al. Cancer Res. 2007 Sep 1;67(17):8014-21. 2. Iwasa T, et al. Clin Cancer Res. 2008 Oct 15;14(20):6496-504. 3. Satoh T, et al. Clin Cancer Res. 2009 Jun 1;15(11):3872-80. 4. Iwasa T, et al. Br J Cancer. 2010 Jun 29;103(1):36-42.
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