LY117018

• 常用名: LY117018
• 英文名: LY 117018
• CAS号: 63676-25-5
• 分子量: 459.55700
• 密度: 1.314g/cm3
• 沸点: 721.5ºC at 760 mmHg
• 分子式: C₂₇H₂₅NO₄S
• 熔点: N/A
• 闪点: 390.2ºC

LY117018用途

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名称

• 英文名: Phenethipylone

LY117018生物活性

• 描述: 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。
• 相关类别:
  信号通路 >> 其他 >> 雌激素受体/ERR
  研究领域 >> 癌症
• 靶点实验:

  Estrogen receptor

• 体外研究: 与在剥离培养基中生长的细胞相比,低浓度(0.01-10nm)的LY117018(0.01-1000nm；24小时)引起p53水平的E2样升高。在较高浓度的LY117018(1μM)下,p53表达水平呈下降趋势。用1μM的LY117018处理导致主要的低磷酸化pRb。在较低浓度下,LY117018不阻断E2诱导的pRb磷酸化[1]。LY117018(1μM；96小时)抑制MCF-7细胞增殖,IC50为1μM[2]。LY117018通过激活ERK1/2信号通路抑制氧化应激诱导的内皮细胞凋亡[3]。细胞增殖实验[2]细胞系：MCF-7细胞浓度：1μM孵育时间：96h结果：IC50为1μM时,MCF-7细胞增殖受到抑制。
• 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.

LY117018物理化学性质

• 密度: 1.314g/cm3
• 沸点: 721.5ºC at 760 mmHg
• 分子式: C₂₇H₂₅NO₄S
• 分子量: 459.55700
• 闪点: 390.2ºC
• 精确质量: 459.15000
• PSA: 98.24000
• LogP: 5.62300
• InChIKey: JLERVPBPJHKRBJ-UHFFFAOYSA-N
• SMILES: O=C(c1ccc(OCCN2CCCC2)cc1)c1c(-c2ccc(O)cc2)sc2cc(O)ccc12
• 折射率: 1.679

LY117018靶点实验

查看更多实验

实验名称：Association constant for estrogen receptor 来源：ChEMBL 靶标：Estrogen receptor beta External Id：CHEMBL675205

实验名称：The compound was tested for anti-uterotrophic activity in immature rats(Dosage 100 ug... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL785932

实验名称：The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1 ug) 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL785933

实验名称：The compound was tested for anti-uterotrophic activity in immature rats(Dosage 10 mic... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL785930

实验名称：Relative binding affinity against Antiestrogen binding site(AEBS) 来源：ChEMBL 靶标：7-dehydrocholesterol reductase External Id：CHEMBL652833

实验名称：The compound was tested for anti-uterotrophic activity in immature rats(Dosage 1000 u... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL785931

实验名称：Inhibition of Calmodulin activation of cyclic nucleotide phosphodiesterase 来源：ChEMBL 靶标：N/A External Id：CHEMBL663190

实验名称：The compound was tested for uterotropic activity in immature rats(Dosage 1000 ug) 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL786490

实验名称：The compound was tested for uterotropic activity in immature rats(Dosage 1 ug) 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL790982

实验名称：The compound was tested for uterotropic activity in immature rats(Dosage 100 ug) 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL790236

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LY117018英文别名

• Methanone,(6-hydroxy-2-(4-hydroxyphenyl)benzo(B)thien-3-yl)(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)
• [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl][4-[2-(1-pyrrolidinyl)ethoxy]phenyl]methanone
• 6-Hydroxy-2-(4-hydroxyphenyl)benzo(B)thien-3-yl 4-(2-(1-pyrrolidinyl)ethoxy) phenyl ketone