YM-155 Hydrochloride

Powder: -20 degree C for 3 years | In solvent: -80 degree C for 1 year

398.85

[Cl-].COCCn1c(C)[n+](Cc2cnccn2)c2c1C(=O)c1ccccc1C2=O

C20H19ClN4O3

(< 1 mg/ml refers to the product slightly soluble or insoluble)

355406-09-6

Sepantronium bromide (YM155; 30uM) does not affect survivin gene promoter-driven luciferase reporter activity but significantly suppresses endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53, by transcriptionally inhibiting the survivin gene promoter. At 100 nM, it does not impact the protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, alpha-actin, and beta-tubulin. Sepantronium bromide demonstrates potent inhibition against various human cancer cell lines, including those with mutated or truncated p53 (e.g., PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5, and A375), with IC50 values ranging between 2.3 to 11 nM. It also increases the sensitivity of NSCLC cells to gamma-radiation, enhancing both the number of apoptotic cells and caspase-3 activity and 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 significant body weight loss and blood cell count reduction. 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 gamma-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].