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Product Description
– 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].
Web ID
– HY-13636S
Shipping
– Room temperature
Molecular Formula
– C32H44D3F5O3S
References
– [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.|[6]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
Molecular Weight
– 609.79
SMILES
– 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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;Autophagy;Estrogen Receptor/ERR;Isotope-Labeled Compounds
Pathway
– Apoptosis;Autophagy;Others;Vitamin D Related/Nuclear Receptor
Product type
– Isotope-Labeled Compounds
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