Etacstil
Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 155701-61-4
- 分子式: C25H22O2
- 分子量:354.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Ishikawa | EC50 |
58 nM
Compound: 6
|
Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells
Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells
|
[PMID: 8201587] |
| MCF7 | EC50 |
0.3 μM
Compound: 3a, GW5638
|
Inhibition of cell proliferation in human MCF7 cells after 7 days by laser scanning imaging cytometer analysis
Inhibition of cell proliferation in human MCF7 cells after 7 days by laser scanning imaging cytometer analysis
|
[PMID: 25790336] |
| MCF7 | EC50 |
0.39 μM
Compound: 4, GW-5638
|
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
|
[PMID: 25879485] |
| MCF7 | EC50 |
390 nM
Compound: GW-5638; 2
|
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
|
[PMID: 30587451] |
| MCF7 | IC50 |
>1.27 μM
Compound: 3a, GW5638
|
Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis
Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis
|
[PMID: 25790336] |
| MCF7 | IC50 |
>100 μM
Compound: 3a, GW5638
|
Agonist activity at ER alpha in human MCF7 cells assessed as PR gene expression after 24 hrs by laser scanning imaging cytometer analysis
Agonist activity at ER alpha in human MCF7 cells assessed as PR gene expression after 24 hrs by laser scanning imaging cytometer analysis
|
[PMID: 25790336] |
| MCF7 | IC50 |
0.985 μM
Compound: 4, GW-5638
|
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
|
[PMID: 25879485] |
| MCF7 | IC50 |
4 μM
Compound: 3a, GW5638
|
Antagonist activity at ER alpha in human MCF7 cells assessed as inhibition of estradiol-induced PR expression treated for 24 hrs after incubation with estradiol for 30 mins by laser scanning imaging cytometer analysis
Antagonist activity at ER alpha in human MCF7 cells assessed as inhibition of estradiol-induced PR expression treated for 24 hrs after incubation with estradiol for 30 mins by laser scanning imaging cytometer analysis
|
[PMID: 25790336] |
| MCF7 | IC50 |
654 nM
Compound: 7a
|
Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha
Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha
|
[PMID: 10673099] |
化学情報
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CAS 番号 155701-61-4
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分子量 354.44
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分子式 C25H22O2
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SMILES
CC/C(C1=CC=CC=C1)=C(C2=CC=CC=C2)/C3=CC=C(C=C3)/C=C/C(O)=O
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別名
DPC974; GW5638
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)