YM-155 hydrochloride

Research use only, not for human use.

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

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.

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.

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.

YM155 hydrochloride | YM 155 hydrochloride

Apoptosis

IAP

IAP

Cancer

Blood cancer

355406-09-6

398.8429

C20H19ClN4O3

>98% (HPLC)

10 mM in DMSO

CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Cl-]

1H-Naphth[2,3-d]imidazolium, 4,9-dihydro-3-(2-methoxyethyl)-2-methyl-4,9-dioxo-1-(2-pyrazinylmethyl)-, chloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years