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)
产品描述 Fulvestrant(同义名:ICI 182780, ZD 182780, ZD 9238, ZM 182780, Faslodex®)是一种新型的Estrogen receptor(ER)(雌***受体)抑制剂,IC50为0.094 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GH3和MMQ细胞增殖[2]。ICI 182780比4OH-***更有效地抑制雌***受体阳性(ER+)乳腺癌细胞增殖[3]。ICI 182780与ER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
化学特性
储存液配制
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). |