Fulvestrant
Cat. No.:YN481286
产品名称: | Fulvestrant |
CAS No.: | 129453-61-8 |
Chemical Name: | 7α-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3,17β-diol |
Synonyms: | 氟维司群; ICI 182780; ZD 9238; ZM 182780 |
分子量: | 606.77 |
分子式: | C₃₂H₄₇F₅O₃S |
SMILES: | C[C@@]12[C@@H](O)CC[C@@]1([H])[C@]3([H])[C@H](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)CC4=C(C=CC(O)=C4)[C@@]3([H])CC2 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Fulvestrant (ICI 182780) 是一种纯抗雌激素,也是一种有效的雌激素受体 (ER) 拮抗剂,IC50为 9.4 nM。Fulvestrant 有效抑制ER阳性 MCF-7 细胞的生长,IC50为 0.29 nM。Fulvestrant 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),并具有抗肿瘤功效。 |
IC50和靶点: | |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Kansra, S., Yamagata, S., Sneade, L., et al.Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin releaseMol. Cell Endocrinol.239(1-2),27-36(2005)
Wardell, S.E., Marks, J.R., and McDonnell, D.P.The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacyBiochem. Pharmacol.82(2),122-130(2011)
Wakeling, A.E., Dukes, M., and Bowler, J.A potent specific pure antiestrogen with clinical potentialCancer Res.51(15),3867-3873(1991)
Zhao, L., O'Neill, K., and Brinton, R.D.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 profileJ. Pharmacol. Exp. Ther.319(3),1124-1132(2006)