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.
For research use only. We do not sell to patients.
- CAS No.: 1316849-17-8
- Formula: C32H47F5O3S
- Molecular Weight:606.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:MMQ prolactinoma cells
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Concentration:1-625 nM
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Incubation Time:72 h
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Result:Decreased expression of activated phosphorylated ERK1/2, JNK, and p38 proteins in MMQ cells in a dose-dependent manner.
Showed no effect on total non-phosphorylated ERK1/2, JNK, or p38 protein levels.
Reduced the p-ERK1/2/β-actin ratio from 0.81 in controls to 0.14 at 625 nM.
Reduced the p-JNK/β-actin ratio from 0.92 in controls to 0.26 at 625 nM.
Reduced the p-p38/β-actin ratio from 0.9 in controls to 0.31 at 625 nM.
Chemical Information
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CAS No. 1316849-17-8
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Molecular Weight 606.77
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Formula C32H47F5O3S
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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
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Synonyms
ICI 182780 (S enantiomer); ZD 9238 (S enantiomer); ZM 182780 (S enantiomer)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fulvestrant (S enantiomer) Related Classifications
HY-13636A Related Classifications
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- Fulvestrant (S enantiomer)
- 1316849-17-8
- ICI 182780 (S enantiomer)
- ZD 9238 (S enantiomer)
- ZM 182780 (S enantiomer)
- Drug Isomer
- Estrogen Receptor/ERR
- p38 MAPK
- Apoptosis
- MMQ prolactinoma cells
- osteocalcin
- breast cancer
- MAPK pathway
- alkaline phosphatase
- apoptosis
- osteoprecursor cell
- ovarian follicle
- prolactinoma
- estrogen receptor
- Inhibitor
- inhibitor
- inhibit