受注:045-509-1970 |
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Synonyms | ICI-182780, ZD 9238, ZM 182780 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C32H47F5O3S |
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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) |
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* <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. |
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。 |
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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. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. [1] Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant 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 Fulvestrant with ER finally results in accelerated degradation of the ER protein. [2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. [5] Fulvestrant 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 Fulvestrant 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 Fulvestrant. [1] Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. [7] Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. [8] |
細胞アッセイ | 細胞株 | MCF-7 breast cancer cells |
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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 |
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]
Macrophages Promote Subtype Conversion and Endocrine Resistance in Breast Cancer [ Cancers (Basel), 2024, 16(3)678] | PubMed: 38339428 |
Testing Adaptive Therapy Protocols Using Gemcitabine and Capecitabine in a Preclinical Model of Endocrine-Resistant Breast Cancer [ Cancers (Basel), 2024, 16(2)257] | PubMed: 38254748 |
Cholesterol biosynthesis inhibition synergizes with AKT inhibitors in triple-negative breast cancer [ bioRxiv, 2024, 10.1101/2024.01.16.575899] | PubMed: none |
Novel Estrogen Receptor Dimerization BRET-Based Biosensors for Screening Estrogenic Endocrine-Disrupting Chemicals [ Biomater Res, 2024, 28:0010] | PubMed: 38464469 |
Short-term tamoxifen administration improves hepatic steatosis and glucose intolerance through JNK/MAPK in mice [ Signal Transduct Target Ther, 2023, 8(1):94] | PubMed: 36864030 |
Cell facilitation promotes growth and survival under drug pressure in breast cancer [ Nat Commun, 2023, 14(1):3851] | PubMed: 37386030 |
N-acetylcysteine overcomes NF1 loss-driven resistance to PI3Kα inhibition in breast cancer [ Cell Rep Med, 2023, 4(4):101002] | PubMed: 37044095 |
Co-targeting RANK pathway treats and prevents acquired resistance to CDK4/6 inhibitors in luminal breast cancer [ Cell Rep Med, 2023, 4(8):101120] | PubMed: 37451269 |
Co-targeting RANK pathway treats and prevents acquired resistance to CDK4/6 inhibitors in luminal breast cancer [ Cell Rep Med, 2023, 4(8):101120] | PubMed: 37451269 |
CCNE1 and PLK1 Mediate Resistance to Palbociclib in HR+/HER2- Metastatic Breast Cancer [ Clin Cancer Res, 2023, 29(8):1557-1568] | PubMed: 36749874 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。