YM155

Cas No.:	781661-94-7
Chemical Name:	1H-Naphth[2,3-d]imidazolium, 4,9-dihydro-1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(2-pyrazinylmethyl)-, bromide (1:1)
Synonyms:	YM-155,YM 155
SMILES:	CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
Formula:	C20H19BrN4O3
M.Wt:	443.29
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	YM-155 is a survivin inhibitor with an IC50 of 0.54 nM.
In Vivo:	YM155 (3 and 10 mg/kg) inhibits the tumor growth in PC-3 xenografts, without obvious body weight loss and blood cell count decrease. YM155 is highly distributed to tumor tissue in vivo. YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts[1]. 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, YM155 and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images[3].
In Vitro:	YM155 (30 μM) is not sensitive to survivn gene promoter-driven luciferase reporter activity. YM155 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. YM155 (100 nM) does not affect protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin. YM155 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]. YM155 resultin in an increase in sensitivity of NSCLC cells to γ-radiation. YM155 combined with γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. In addition, YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA[2].