Fulvestrant (S enantiomer)  (Synonyms: ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer))

Fulvestrant (ICI 182780; ZD 9238) S enantiomer is the S-enantiomer of Fulvestrant (HY-13636), a potent estrogen receptor inhibitor. Fulvestrant binds to and blocks the estrogen receptor, promotes its degradation, and thereby inhibits receptor dimerization, nucleocytoplasmic shuttling and transcriptional activity. Fulvestrant effectively blocks estrogen signaling, MAPK pathway activation and ER-regulated protein expression. Fulvestrant induces apoptosis, inhibits the proliferation of breast cancer and prolactinoma cells, and reduces the mineralization level, alkaline phosphatase activity and osteocalcin expression of preosteoblasts. Prenatal exposure to Fulvestrant impairs ovarian follicular development and causes ovarian structural damage. Fulvestrant has been widely used in studies related to breast cancer, prolactinoma and other conditions^[1][2][3][4].

Fulvestrant (5-625 nM; 72 h) inhibits the proliferation of MMQ prolactinoma cells in a dose-dependent manner, with an IC₅₀ of 32.4 nM after 72 h of treatment^[1].
Fulvestrant (1-625 nM; 72 h) dose-dependently promotes apoptosis of MMQ prolactinoma cells, with the total apoptosis rate reaching 84.21% at 625 nM^[1].
Fulvestrant (1-625 nM; 72 h) for 72 hours dose-dependently inhibits the activation of MAPK pathway proteins p-ERK1/2, p-JNK, and p-p38 in MMQ prolactinoma cells, without altering the total MAPK protein levels^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

606.77

C₃₂H₄₇F₅O₃S

1316849-17-8

C[C@@]12[C@@H](O)CC[C@@]1([H])[C@]3([H])[C@H](CCCCCCCCC[S@@](CCCC(F)(F)C(F)(F)F)=O)CC4=C(C=CC(O)=C4)[C@@]3([H])CC2

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• [1]. Li C, et al. Effects of fulvestrant, an estrogen receptor antagonist, on MMQ cells and its mechanism. Neuro Endocrinol Lett. 2009;30(2):268-274.

  [2]. Park JB, et al. The effects of fulvestrant, an estrogen receptor antagonist, on the proliferation, differentiation and mineralization of osteoprecursor cells. Mol Med Rep. 2013;7(2):555-558.

  [3]. Sulaymanova R T. Effect of the prenatal action of fulvestrant on the ovaries of the offspring of laboratory mice[J]. RUDN Journal of Medicine, 2021, 25(3): 256-262.

  [4]. Osborne CK, et al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004;90 Suppl 1(Suppl 1):S2-S6.  [Content Brief]