LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines.
LY117018 (0.01-1000 nM; 24 hours) at lower concentrations (0.01-10 nM) caused an E2-like increase in p53 levels when compared to its effects on cells grown in the stripped medium. At a higher concentration of LY117018 (1 μM), the level of p53 appeared to decline. Treatment with 1 μM LY117018 resulted in a predominantly pophosphorylated pRb. At lower concentrations, LY117018 did not block E2-induced pRb phosphorylation[1].LY117018 (1 μM; 96 hours) inhibits MCF-7 cells proliferation with an IC50 of 1 μM[2].LY117018 suppresses oxidative stress-induced endothelial cell apoptosis through activation of ERK1/2 signaling pathway[3].
References:
[1]. Dinda S, et al. Effects of LY117018 (a SERM analog of raloxifene) on tumor suppressor proteins and proliferation of breast cancer cells.Horm Mol Biol Clin Investig. 2010 Aug 1;2(1):211-7.
[2]. Baumann KH, et al. Effects of celecoxib and ly117018 combination on human breast cancer cells in vitro.Breast Cancer (Auckl). 2009 Apr 7;3:23-34.
[3]. Yu J, et al.Raloxifene analogue LY117018 suppresses oxidative stress-induced endothelial cell apoptosis through activation of ERK1/2 signaling pathway.Eur J Pharmacol. 2008 Jul 28;589(1-3):32-6.