Fulvestrant-d3

Fulvestrant-d3 is the deuterium labeled 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].

ICI 182780-d3; ZD 9238-d3; ZM 182780-d3

12352005

Apoptosis; Autophagy; Estrogen Receptor/ERR; Isotope-Labeled Compounds

Isotope-Labeled Compounds

Apoptosis; Autophagy; Others; Vitamin D Related/Nuclear Receptor

Cancer

97.6

DMSO : 250 mg/mL (ultrasonic; warming)

C[C@@]12[C@](O)([2H])C([2H])([2H])C[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

C32H44D3F5O3S

609.79

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]Wakeling AE, et al. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991 Aug 1;51 (15) :3867-73.|[3]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.|[4]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|[5]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.|[6]Julia Kuhn, et al. GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. Eur J Neurosci. 2008 Apr;27 (7) :1700-9.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Isotope-Labeled Compounds