Fulvestrant (estrogen receptor inhibitor)
英文名称: Fulvestrant (estrogen receptor inhibitor)
型号:null    产品货号: IHR1021-0005MG
价格:请致电:010-57128832,18610462672
品牌: gene operation

 IHR1021-Fulvestrant

Fulvestrant>99%

【英文同义名】:ICI 182780, ZD 182780, ZD 9238, ZM 182780, Faslodex®

【中文同义名】:

订购信息:(原装进口,常备现货)

 

产品名称

产品货号

目录价(元)

Gene Operation

Fulvestrant (estrogen receptor inhibitor

IHR1021-0005MG

5MG

¥979.00

IHR1021-0025MG

25MG

¥4,029.00

产品描述

Fulvestrant(同义名:ICI 182780, ZD 182780, ZD 9238, ZM 182780, Faslodex®)是一种新型的Estrogen receptorER)(雌***受体)抑制剂,IC500.094 nM。在临床前模型和临床实验中缺少雌***激动剂活性。ICI 182780能抑制乳腺癌生长,目前已用于晚期乳腺癌的III期临床研究中[1]ICI 182780也是泌乳素分泌细胞的强效抑制剂,抑制GH3MMQ细胞增殖[2]ICI 1827804OH-***更有效地抑制雌***受体阳性(ER+)乳腺癌细胞增殖[3]ICI 182780ER结合,导致肿瘤中ER蛋白快速减少。这种ER浓度的下调是剂量依赖型的,同时肿瘤孕***受体(PgR)浓度也显著减少[4]

靶点

靶点

ER

IC50(半数有效浓度)

0.094 nM

化学特性

Cas No.: 129453-61-8

分子量: 606.77

分子式: C32H47F5O3S

纯度: >99% 

同义名: ICI 182,780, ZD 182780, ZD 9238, ZM 182780, Faslodex®

化学名:,-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]estra-1,3,5(10 )- triene-3,17β-diol

外观: 白色粉末

溶解: 溶于DMSO(up to 100 mg/mL)

保存:3 -20 粉末

储存液配制

储存液 (1 ml DMSO体系)

1 mM

5 mM

10 mM

25 mM

50 mM

100 mM

质量(mg)

0.6068

3.0339

6.0677

15.1693

30.3850

60.6770

结构式

使用浓度(仅作参考)

Fulvestrant的具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。

参考文献

[1] Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 51(15):3867-73 (1991).

[2] de Cupis A, et al. Comparison between novel steroid-like and conventional nonsteroidal antioestrogens in inhibiting oestradiol- and IGF-I-induced proliferation of human breast cancer-derived cells. Br J Pharmacol. 116(5): 2391–2400 (1995).

[3] Howell, et al. ICI 182,780 (FaslodexTM): Development of a novel, "pure" antiestrogen. Cancer 89: 817-825(2000).

[4] Thomas P, et al. Identity of an Estrogen Membrane Receptor Coupled to a G Protein in Human Breast Cancer Cells. Endocrinology. 146(2):624-32 (2005).

[5] Zhao L, et al. Estrogenic agonist activity of ICI 182,780 (Faslodex) in hippocampal neurons: implications for basic science understanding of estrogen signaling and development of estrogen modulators with a dual therapeutic profile. J Pharmacol Exp Ther. 319(3):1124-32 (2006).