ERα degrader 7
ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research.
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- 分子式: C28H24F4N2O3
- 分子量:512.50
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
IC50: 14.6 nM (ERα)[1]
体外実験
ERα degrader 7 (10-5-10 μM, 5 d) demonstrates antitumor activity against the breast cancer cell (IC50 = 4.21 nM) and noncytotoxicity against normal breast epithelial cell[1].
ERα degrader 7 (50-1000 nM, 5 d) shows a significant concentration-dependent degradation effect of ERα in MCF-7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-10 (normal breast epithelial cell)
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Concentration:10-5-10 μM
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Incubation Time:5 d
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Result:Demonstrated low inhibition against MCF-10A, cell proliferation rate of each concentration are all above 80%.
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Cell Line:MCF-7 (breast cancer cell)
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Concentration:10-5-10 μM
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Incubation Time:5 d
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Result:ERα degrader 7 (10-3-10 μM) demonstrated excellent antitumor activity against the MCF-7 cell, caused an inhibition rate ranged from 60% to 75%, results were evaluated using GDC-9545 as a positive control.
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Cell Line:MCF-7 (breast cancer cell)
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Concentration:1, 10, 50, 100, 200, 500, 1000 nM
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Incubation Time:5 d
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Result:Showed a concentration-dependent degradation effect of ERα. Demonstrated a significant ERα-degradation effect (ERα expression rate < 50%) at a concentration of 50 nM, results were evaluated using GDC-9545 as a positive control.
化学情報
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分子量 512.50
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分子式 C28H24F4N2O3
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SMILES
OC(C1=CC=C(C2=CC(F)=C([C@@H]3C(NC4=CC=CC=C45)=C5C[C@@H](C)N3CC(F)(F)CO)C(F)=C2)C=C1)=O
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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)
ERα degrader 7 関連分類
HY-155492 関連分類
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