Fulvestrant

Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].

Product Specifications

CAS Number

[129453-61-8]

Product Name Alternative

ICI 182780; ZD 9238; ZM 182780

UNSPSC

12352005

Hazard Statement

H303, H315, H360, H362, H410

Target

Apoptosis; Autophagy; Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Fulvestrant.html

Purity

99.95

Solubility

DMSO : 250 mg/mL (ultrasonic)

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

Molecular Formula

C32H47F5O3S

Molecular Weight

606.77

Precautions

H303, H315, H360, H362, H410

References & Citations

[1]Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51 (15) :3867-73.|[2]Osborne CK, et al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1:S2-6.|[3]Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26 (9) :948-56|[4]Yu X, et al.MiR-214 increases the sensitivity of breast cancer cells to tamoxifen and fulvestrant through inhibition of autophagy.Mol Cancer. 2015 Dec 15;14:208.|[5]Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27 (7) :1700-9.