Fulvestrant

• Description:

  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 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• CAS Number:

  [129453-61-8]