LY117018

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LY117018 

LY117018,Raloxifene 类似物,是一种选择性雌激素受体 (estrogen receptor) 调节剂。LY117018 对乳腺癌细胞具有抗增殖作用。

LY117018

LY117018 Chemical Structure

CAS No. : 63676-25-5

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生物活性

LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines[1][2].

IC50 & Target[1]

Estrogen receptor

 

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: MCF-7 cells
Concentration: 1 μM
Incubation Time: 96 hours
Result: Inhibited MCF-7 cells proliferation with an IC50 of 1 μM.

分子量

459.56

Formula

C27H25NO4S

CAS 号

63676-25-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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