Fulvestrant ici 182780
Fulvestrant - AstraZeneca Alternative Names: Faslodex; ICI 182780; ZD 182780; ZD 9238; ZM 182780 Latest Information Update: 05 Aug 2020
Fulvestrant treatment caused a significant decrease in MDM2 protein expression in human breast cancer cell lines MCF7 and T47D, and that the reduction of MDM2 APExBIO - Fulvestrant (ICI 182,780)|Estrogen receptor antagonist,high affinity|CAS# 129453-61-8 Howell A, Robertson J F R, Quaresma Albano J, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment[J]. Journal of Clinical Oncology, 2002, 20(16): 3396-3403. Fulvestrant (ICI … This study proposed to investigate further the role of oestrogens during pubertal growth of rat ventral prostate, by analysing the effect of anti-oestrogen fulvestrant (ICI 182,780) on the expression of androgen (AR) and oestrogen receptors (ESR1 and ESR2), mitogen-activated protein kinase (ERK1/2) phosphorylation, and expression of Ki-67, a biomarker for cell proliferation.
20.12.2020
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. 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. For research use only. Fulvestrant (ICI 182,780) down-regulates androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells Rumi S. Bhattacharyya, Aruna V. Krishnan, Srilatha Swami and David Feldman DOI: 10.1158/1535-7163.MCT-06-0065 Published June 2006 Fulvestrant (ICI-182780) is an estrogen receptor (ER) antagonist with an IC50 of 9.4 nM in a cell-free assay.
22/7/2009
Correlative studies. Drug: Lapatinib Ditosylate. Given PO. Other Name: Tykerb. 15 Mar 2019 ICI 182780 is fulvestrant.
Nov 13, 2000 · ICI 182,780 specifically down‐regulates the estrogen receptor and, thus, represents the first of a new class of therapeutic agents. In this report, the authors present the current evidence that distinguishes ICI 182,780 from tamoxifen and related nonsteroidal compounds and establishes ICI 182,780 as the first in a new class of therapeutic agents.
with AZ’s Faslodex fulvestrant, which is injected twice monthly and doesn’t always reach the tumor. Faslodex..Epidermal growth factor receptor 2 Danielle Golovin OP-1250 Tagrisso (Brand), AZD9291 (Compound #), osimertinib (Generic), Tagrisso (Other) Faslodex, fulvestrant (ICI 182,780) AstraZeneca Fulvestrant-d3: Synonyms (7α,17β)-7-[9-[4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol-d3; Faslodex-d3; Fulvestrant-d3; ICI 182780-d3; ZD 182780-d3; ZD 9238-d3; ZM 182780-d3; Alternate CAS # unlabelled: 129453-61-8: Molecular Formula: C₃₂H₄₄D₃F₅O₃S: Appearance: White to Off-White Solid: Melting Point In rats, treatment with fulvestrant (ICI 182,780), a steroidal antiestrogen that impairs estrogen action on both ESR1 and ESR2 and does not cross the blood-brain barrier , causes morphological and functional changes in the efferent ductules similar to those seen in the Esr1 −/− mice, including luminal dilation and reduction of the epithelial height, that ultimately lead to testicular 1. J Pharmacol Exp Ther. 2002 Aug;302(2):584-93.
Howell A, Robertson J F R, Quaresma Albano J, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment[J]. Journal of Clinical Oncology, 2002, 20(16): 3396-3403.
Abstract ICI 182,780 is one of a new class of steroidal antiestrogens that differs from nonsteroidal antiestrogens, such as tamoxifen, in a number of respects. 1) It is bound by estrogen receptors with a high affinity, similar to that for estradiol. 2) It is a "pure" antiestrogen in that it does not mimic any of the effects of estradiol. DRUG NAME: Fulvestrant SYNONYM(S): ICI -182780; ZD 92381. COMMON TRADE NAME(S): FASLODEX® CLASSIFICATION: hormonal agent. Special pediatric considerations are noted when applicable, otherwise adult provisions apply. MECHANISM OF ACTION: Fulvestrant is an estrogen receptor antagonist with no partial agonist effects, including its effects on the Nov 13, 2000 · ICI 182,780 specifically down‐regulates the estrogen receptor and, thus, represents the first of a new class of therapeutic agents.
ICI 182,780 (Faslodex™) from AstraZeneca (Cheshire, United Kingdom) is a novel, steroidal estrogen antagonist that was designed to be devoid of estrogen agonist activity in preclinical models. 7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)estra-1,3,5(10)-triene-3,17-diol | faslodex | fulvestrant | ici 182780 | ici 182,780 | ici-182780 | zd9238 | zd-9238 | zm 182780 | zm-182780 Feedback Data collection and curation is an ongoing process for CDEK - if you notice any information here to be missing or incorrect, please let us know! Literature References: Novel steroidal estrogen antagonist reported to lack any partial agonist activity. Prepn: J. Bowler, B. S. Tait, EP 138504; eidem, US 4659516 Synonyms: Fulvestrant, ICI-182780, ZD 9238, Faslodex Hazardous Ingredient: Fulvestrant (ICI-182780) CAS Registry Number: 129453-61-8 Molecular Weight: 606.77 Molecular Formula: C 32 H 47 F 5 O 3 S 3. HAZARDS IDENTIFICATION: Hazard Description: Substance not fully tested 4.
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. 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. For research use only. Fulvestrant (ICI 182,780) down-regulates androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells Rumi S. Bhattacharyya, Aruna V. Krishnan, Srilatha Swami and David Feldman DOI: 10.1158/1535-7163.MCT-06-0065 Published June 2006 Fulvestrant (ICI-182780) is an estrogen receptor (ER) antagonist with an IC50 of 9.4 nM in a cell-free assay.
In this study we tested the hypothesis that fulvestrant induces specific nuclear matrix protein-ERα interactions that mediate receptor immobilization and turnover. A glutathione S-transferase (GST)-ERα Fulvestrant (ICI 182,780) sensitizes breast cancer cells expressing estrogen receptor α to vinblastine and vinorelbine. Donghai Jiang. Breast Cancer Res Treat DOI 10 The main family of selective estrogen antagonists are steroids bearing a long lipophilic chain at C-6, represented by ICI-164384 and fulvestrant (ICI-182780, Faslodex®), the latter of which was approved in 2002 for the treatment of hormone-positive metastatic breast cancer. 20, 21 Cells were maintained in a humidified atmosphere at 37°C and 95% air/5% CO 2.
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6/1/2004
In this study we tested the hypothesis that fulvestrant induces specific nuclear matrix protein-ERα interactions that mediate receptor immobilization and In this study, we investigated the effects of a new estrogen-blocking agent, Faslodex (ICI 182,780), on estrogen-accelerated skeletal maturation in immature mice. On day-of-life 2 through 8, mice pups received either estradiol (5 microg/100 g body weight), Faslodex (100 microg/100 g body weight), a combination of Faslodex + estradiol, or A high affinity estrogen receptor antagonist (IC 50 = 0.29 nM), devoid of any partial agonism both in vitro and in vivo. Also high affinity agonist at the membrane estrogen receptor GPER.
Synonyms: Faslodex® | ICI 182,780 | ICI 182780 | ICI182780 | ZD-9238. Approved drug. fulvestrant is an approved drug (FDA (2002), EMA (2004)). Compound
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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. For research use only. [3]. Howell A, Robertson J F R, Quaresma Albano J, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment[J].