1316849-17-8
Chemical Structure
Fulvestrant (S enantiomer)
Synonym(s): ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer)
- CAS No.: 1316849-17-8
- Formula:C32H47F5O3S
- Molecular Weight:606.77
IUPAC Name: (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((S)-(4,4,5,5,5-pentafluoropentyl)sulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
InChIKey: VWUXBMIQPBEWFH-GXZKXCMSSA-N
SMILES: 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
Biological Activity: 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].
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Fulvestrant (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. | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [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]
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