Fulvestrant-d3(Synonyms: ICI 182780-d3; ZD 9238-d3; ZM 182780-d3)

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Fulvestrant-d3 (Synonyms: ICI 182780-d3; ZD 9238-d3; ZM 182780-d3)

Fulvestrant-d3 (ICI 182780-d3) 是 Fulvestrant 的氘代物。Fulvestrant (ICI 182780) 是一种纯抗雌激素，也是一种有效的雌激素受体 (ER) 拮抗剂，IC50 为 9.4 nM。Fulvestrant 还是一种 GPR30 的激动剂。Fulvestrant 有效抑制 ER 阳性 MCF-7 细胞的生长，IC50 为 0.29 nM。

Fulvestrant-d3(Synonyms: ICI 182780-d3; ZD 9238-d3; ZM 182780-d3)

Fulvestrant-d3 Chemical Structure

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生物活性

Fulvestrant-d3 (ICI 182780-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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

609.79

Formula

C32H44D3F5O3S
中文名称

氟维司群 d3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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