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Fulvestrant
別名：ICI-182780, ZD 9238, ZM 182780
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。
CAS No. 129453-61-8
文献中Selleckの製品使用例（169）
製品安全説明書
現在のバッチを見る：
純度：
99.97%
99.97
Fulvestrant関連製品
Estrogen/progestogen Receptor阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| A549 | Growth Inhibition Assay | 5 μM | 72 h | inhibits cell growth significantly combined with vandetanib | 22258476 |
| 201T | Growth Inhibition Assay | 5 μM | 72 h | inhibits cell growth significantly combined with vandetanib | 22258476 |
| Huh7 | Function Assay | 50 μM | 48 h | inhibits genistein-mediated PON1 transactivation | 22304296 |
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
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。 | ||
|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| 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] | |||
|---|---|---|---|---|
| 細胞実験 | 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. | |||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | MDM2 / ER p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK ErbB3 ERα |
|
24747123 | |
| Immunofluorescence | IGF-1R / Erα Snail / E-cadherin |
|
19815064 | |
| Growth inhibition assay | Cell viability |
|
29787591 | |
| In Vivo | ||
| 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] | |
|---|---|---|
| 動物実験 | 動物モデル | The human breast cancer xenografts MCF-7 in nude mice |
| 投与量 | 5 mg/mouse | |
| 投与経路 | s.c. injection | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06239467 | Recruiting | Advanced Cancer|Breast Cancer |
OnKure Inc. |
March 1 2024 | Phase 1 |
| NCT06257264 | Recruiting | Breast Cancer|Small Cell Lung Cancer|Ovarian Cancer|Gastric Cancer|Hormone-receptor-positive Breast Cancer|Hormone Receptor Positive HER-2 Negative Breast Cancer|Advanced Solid Tumor|Endometrial Cancer|Prostate Cancer |
BeiGene |
February 28 2024 | Phase 1 |
| NCT05905341 | Withdrawn | Breast Cancer|Ovarian Cancer|Liposarcoma|Non-small Cell Lung Cancer (NSCLC)|Endometrial|Solid Tumors |
Pfizer |
January 15 2024 | Phase 1 |
| NCT05963984 | Recruiting | Metastatic Breast Cancer|Locally Advanced Breast Cancer|Breast Cancer |
Carrick Therapeutics Limited|Pfizer |
December 14 2023 | Phase 2 |
| NCT06129786 | Recruiting | Breast Cancer |
Centro di Riferimento Oncologico - Aviano |
May 18 2023 | -- |
化学情報
| 分子量 | 606.77 | 化学式 | C32H47F5O3S |
| CAS No. | 129453-61-8 | SDF | Download Fulvestrant SDFをダウンロードする |
| Smiles | CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F | ||
| 保管 | |||
|
In vitro |
DMSO : 100 mg/mL ( (164.8 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 100 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
| Clear solution |
5% DMSO
95% Corn oil
|
1.25mg/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. | ||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問1:
Is there any information for the half-life of fulvestrant (Cat No.S1191)?
回答
S1191, is about 13.5 to 18.5 hours in vivo: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2750771/. The half life of these compounds in cell culture might be different and we generally recommend replenishing with fresh drug every 24-48 hours.
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