LY117018 TFA, an analog of Raloxifene, functions as a selective estrogen receptor modulator and demonstrates antiproliferative effects on breast cancer cell lines [1] [2] [3].

LY117018, at low concentrations (0.01-10 nM), increases p53 levels in comparison to cells grown in stripped medium, akin to the effect of E2. When LY117018 is at a higher concentration (1 μM), p53 levels appear to decrease. Treatment with 1 μM LY117018 results in primarily hypophosphorylated pRb. At low concentrations, LY117018 does not inhibit E2-induced pRb phosphorylation [1]. LY117018 (1 μM; 96 h) inhibits the proliferation of MCF-7 cells with an IC50 of 1 μM [2]. Additionally, LY117018 suppresses oxidative stress-induced endothelial cell apoptosis by activating the ERK1/2 signaling pathway [3].