2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. 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.

ERα degrader 10 Chemical Structure

ERα degrader 10 Chemical Structure

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ERα degrader 10 Related Antibodies

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Description

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[1].

IC50 & Target[1]

ERα

24 nM (IC50)

In Vitro

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.

ERα degrader 10 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.1 nM, 1 nM, 10 nM, 50 nM, 100 nM, 500 nM, 1000 nM
Incubation Time: 1 h, 3 h, 6 h, 12 h, 24 h, 48 h
Result: ERα protein level decreased significantly.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10 nM, 50 nM, 100 nM
Incubation Time: 24 h
Result: Could induce cell cycle arrest in G1 phase.
In Vivo

ERα degrader 10 (10-30 mg/kg; po; daily; for 30 days) shows excellent antitumor effect in the MCF-7 xenograft model in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice injected with MCF-7 cells and estrogen (0.15 mg/mL)[1]
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral gavage; daily; for 30 days
Result: Showed excellent antitumor effect in the MCF-7 xenograft model in vivo
Molecular Weight

468.97

Formula

C29H25ClN2O2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ERα degrader 10 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ERα degrader 10ERα degrader10ERα degrader-10Estrogen Receptor/ERRERα degraderproteasome-mediated pathwaybreast cancerG1 phaseInhibitorinhibitorinhibit

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