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

For research use only. We do not sell to patients.

ERα degrader 7 Chemical Structure

ERα degrader 7 Chemical Structure

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ERα degrader 7 Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Description

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[1].

IC50 & Target

IC50: 14.6 nM (ERα)[1]
In Vitro

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.

ERα degrader 7 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MCF-10 (normal breast epithelial cell)
Concentration: 10-5-10 μM
Incubation Time: 5 d
Result: Demonstrated low inhibition against MCF-10A, cell proliferation rate of each concentration are all above 80%.

Cell Proliferation Assay[1]

Cell Line: MCF-7 (breast cancer cell)
Concentration: 10-5-10 μM
Incubation Time: 5 d
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.

Western Blot Analysis[1]

Cell Line: MCF-7 (breast cancer cell)
Concentration: 1, 10, 50, 100, 200, 500, 1000 nM
Incubation Time: 5 d
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.
Molecular Weight

512.50

Formula

C28H24F4N2O3
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
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 7 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 7ERα degrader7ERα degrader-7Estrogen Receptor/ERRMCF-7MCF-10AERαbreast cancerSERDestrogen-receptordegraderInhibitorinhibitorinhibit

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ERα degrader 7
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HY-155492
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