ERα degrader 10
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer.
For research use only. We do not sell to patients.
- Formula: C29H25ClN2O2
- Molecular Weight:468.97
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ERα 24 nM (IC50) |
ERα degrader 10 (Compound A20) shows outstanding anti-proliferative effects on MCF-7 cells (IC50 = 0.28 nM).
ERα degrader 10 (Compound A20; 0.1-1000 nM; 1-48 h) shows the ERα degradation in a concentration-dependent manner, and the degradation effect is best at 24 h via a proteasome-mediated protein degradation pathway[1].
ERα degrader 10 (10-100 nM; 24 h) could suppress the ERα signal transduction, inducing the MCF-7 cell cycle arrest in G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.1 nM, 1 nM, 10 nM, 50 nM, 100 nM, 500 nM, 1000 nM
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Incubation Time:1 h, 3 h, 6 h, 12 h, 24 h, 48 h
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Result:ERα protein level decreased significantly.
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Cell Line:MCF-7 cells
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Concentration:10 nM, 50 nM, 100 nM
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Incubation Time:24 h
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Result:Could induce cell cycle arrest in G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice injected with MCF-7 cells and estrogen (0.15 mg/mL)[1]
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Dosage:10 mg/kg and 30 mg/kg
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Administration:Oral gavage; daily; for 30 days
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Result:Showed excellent antitumor effect in the MCF-7 xenograft model in vivo
Chemical Information
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Molecular Weight 468.97
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Formula C29H25ClN2O2
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SMILES
O=C(O)/C=C/C1=CC=C(/C(C2=CC=C(C3=CN(C)N=C3)C=C2)=C(C4=CC=CC=C4Cl)/CC)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ERα degrader 10 Related Classifications
HY-168099 Related Classifications
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