Fulvestrant (ICI-182780)

製品コードS1191 バッチS119120

印刷

化学情報

Chemical Structure Synonyms ICI-182780, ZD 9238, ZM 182780 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C32H47F5O3S
分子量 606.77 CAS No. 129453-61-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (164.8 mM)
Ethanol 100 mg/mL (164.8 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.250mg/ml (2.06mM) Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 フルベストラント (Fulvestrant (ICI-182780, ZD 9238, ZM 182780)) はエストロゲン受容体 (estrogen receptor, ER) アンタゴニストであり、cell-free assay における IC50 は 0.94 nM です。フルベストラントはまたオートファジー (autophagy) とアポトーシス (apoptosis) を誘導し、抗腫瘍活性を呈します。
in vitro Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. This compound causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. [1] It competitively inhibits binding of oestradiol to the estrogen receptor. This agent blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of this compound with ER finally results in accelerated degradation of the ER protein. [2] This chemical (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM of this compound leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] It is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. This agent also significantly attenuates R1881-stimulated growth by 70%. [5] It is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. [6]
in vivo Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of this compound suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM this chemical. [1] This compound (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. [7] It also displays anti-angiogenesis in the chick egg chorioallantoic membrane. [8]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 breast cancer cells
濃度 2.9 nM
反応時間 5 days
実験の流れ MCF-7 cells are cultured in multiwell plates (24-well, seeding density 4 × 104) in minimal essential medium containing phenol red, insulin (10 μg/mL), and 5% charcoal-stripped fetal calf serum without additional estradiol. Fulvestrant and/or estradiol are added in fresh medium 2 days after seeding. Cultures are maintained for 5 days with one further medium change and growth is assessed by measurement of total cell protein at the beginning and end of treatment and compared with that of controls treated with ethanol (0.1%) alone.
動物実験 動物モデル The human breast cancer xenografts MCF-7 in nude mice
投薬量 5 mg/mouse
投与方法 s.c. injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/1855205/
  • https://pubmed.ncbi.nlm.nih.gov/15094757/
  • https://pubmed.ncbi.nlm.nih.gov/9816164/
  • https://pubmed.ncbi.nlm.nih.gov/11110059/
  • https://pubmed.ncbi.nlm.nih.gov/16818513/
  • https://pubmed.ncbi.nlm.nih.gov/12832521/
  • https://pubmed.ncbi.nlm.nih.gov/20874728/
  • https://pubmed.ncbi.nlm.nih.gov/7678775/

カスタマーフィードバック

Data from [Data independently produced by Mol Cancer Ther, 2014, 13(1), 230-8]

Data from [PLoS One, 2011, 6, e21112]

Data from [PLoS One, 2011, 6, e21112]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Dual targeting CDK4/6 and CDK7 augments tumor response and anti-tumor immunity in breast cancer models [ J Clin Invest, 2025, e188839] PubMed: 40794455
Combined inhibition of KAT6A/B and Menin reverses estrogen receptor-driven gene expression programs in breast cancer [ Cell Rep Med, 2025, 6(7):102192] PubMed: 40516531
A bedside-to-bench translational analysis of NF1 alterations and CDK4/6 inhibitor resistance in hormone receptor-positive metastatic breast cancer [ EBioMedicine, 2025, 118:105828] PubMed: 40578027
Blocking cancer-fibroblast mutualism inhibits proliferation of endocrine therapy resistant breast cancer [ Mol Syst Biol, 2025, 10.1038/s44320-025-00104-6] PubMed: 40341770
Selective degradation of FGFR1/2 overcomes antiestrogen resistance in ER+ breast cancer with FGFR1/2 alterations [ Cancer Lett, 2025, 619:217668] PubMed: 40127812
Targeting estrogen-regulated system xc- promotes ferroptosis and endocrine sensitivity of ER+ breast cancer [ Cell Death Dis, 2025, 16(1):30] PubMed: 39833180
Oestrogen Receptor Alpha in Myocyte Maintains Muscle Regeneration in Duchenne Muscular Dystrophy [ J Cachexia Sarcopenia Muscle, 2025, 16(2):e13807] PubMed: 40258782
Annotation-free deep learning algorithm trained on hematoxylin & eosin images predicts epithelial-to-mesenchymal transition phenotype and endocrine response in estrogen receptor-positive breast cancer [ Breast Cancer Res, 2025, 27(1):6] PubMed: 39800743
Progranulin deficiency associates with postmenopausal osteoporosis via increasing ubiquitination of estrogen receptor α [ Genes Dis, 2025, 12(1):101221] PubMed: 39559258
Co-targeting of metabolism using dietary and pharmacologic approaches reduces breast cancer metastatic burden [ NPJ Breast Cancer, 2025, 11(1):3] PubMed: 39809806

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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