YM155 (Sepantronium bromide) is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity. YM155 also completely inhibited the growth of orthotopically xenografted PC-3 tumors. YM155 suppressed expression of survivin and induced apoptosis in PC-3 and PPC-1 human HRPC cell lines at 10 nmol/L. It selectively suppresses expression of survivin and induces apoptosis in p53-deficient cancer cells in vitro at 10 nM. YM155 is highly distributed to tumors and at concentrations approximately 20-fold higher than those in plasma. YM155 exerts anti-tumor effects in various in vivo cancer models, including prostate, pancreatic, and lung cancer.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL
Water 80 mg/mL
|Source||J Transl Med (2018). Figure 2. YM155|
|Method||Cell viability assay|
|Cell Lines||U251 and U87 cells|
|Incubation Time||48 h|
|Results||Cell viability decreased significantly in cells treated with both radiation and YM155 (5 nM) compared to radiation alone|
Radiosensitizing effect of YM155, a novel small-molecule survivin suppressant, in non-small cell lung cancer cell lines.
Iwasa T, et al. Clin Cancer Res. 2008 Oct 15;14(20):6496-504. PMID: 18927289.
YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts.
Nakahara T, et al. Cancer Res. 2007 Sep 1;67(17):8014-21. PMID: 17804712.
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