For research use only. Not for therapeutic Use.
LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines[1][2].
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 hypophosphorylated 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].
| Catalog Number | R045570 |
| CAS Number | 63676-25-5 |
| Synonyms | [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]methanone |
| Molecular Formula | C27H25NO4S |
| Purity | ≥95% |
| InChI | InChI=1S/C27H25NO4S/c29-20-7-3-19(4-8-20)27-25(23-12-9-21(30)17-24(23)33-27)26(31)18-5-10-22(11-6-18)32-16-15-28-13-1-2-14-28/h3-12,17,29-30H,1-2,13-16H2 |
| InChIKey | JLERVPBPJHKRBJ-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O |
| Reference | [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. |
