ERα degrader 6
ERα degrader 6 is a selective dual-targeting estrogen receptor α (ERα) degrader. ERα degrader 6 induces ERα degradation, aromatase inhibition, and exerts antiproliferative effects in endocrine-resistant breast cancer cells. ERα degrader 6 can be used for research related to endocrine-resistant breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2775441-10-4
- Formula: C28H23F3N4O4S
- Molecular Weight:568.57
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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
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.14 μM
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Antiproliferative activity against human MCF-7 ER+ breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Antiproliferative activity against human MCF-7 ER+ breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
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37037140 |
| MCF-10A | IC50 |
26.33 μM
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Cytotoxicity against human MCF-10A normal breast cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
Cytotoxicity against human MCF-10A normal breast cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay.
|
37037140 |
In Vitro
ERα degrader 6 binds with moderate affinity to ERα and shows 10-fold selectivity for ERα over ERβ, with a Ki of 0.075 μM for ERα[1].
ERα degrader 6 inhibits human aromatatase activity with an IC50 of 37.73 nM[1].
ERα degrader 6 (24 h) acts as an ERα antagonist in HEK293T cells, with an EC50 of 3.96E-08 M and 15% efficacy relative to Estradiol (HY-B0141)[1].
ERα degrader 6 (0.5-10 μM; 24 h) induces ERα degradation in MCF-7 cells in vitro in a concentration-dependent manner[1].
ERα degrader 6 (0.5-10 μM; 24 h) induces ERα degradation in LCC2 Tamoxifen-resistant breast cancer cells in a concentration-dependent manner[1].
ERα degrader 6 inhibits ESR1 transcription in MCF-7 breast cancer cells, reducing mRNA levels to ~70% of control[1].
ERα degrader 6 binds to the ERα LBD via specific hydrogen bonds and helix 11 interactions, supporting its SERD activity[1].
ERα degrader 6 binds to human aromatase via specific hydrogen bonds and a sulfonamide oxygen-heme iron coordination bond, supporting its aromatase inhibitory activity[1].
ERα degrader 6 (31q) (72 h) potently inhibits the proliferation of MCF-7 ER+ breast cancer cells (IC50 = 0.14 μM), inhibits Tamoxifen (HY-13757A)-resistant LCC2 breast cancer cells (IC50 = 8.82 μM), and shows low toxicity to normal MCF-10A breast cells (IC50 = 26.33 μM)[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 breast cancer cells
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Concentration:0.5-10 μM; 5 μM (with 10 μM MG132)
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Incubation Time:24 h
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Result:Induced ERα degradation in MCF-7 cells in a concentration-dependent manner.
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Cell Line:LCC2 tamoxifen-resistant breast cancer cells
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Concentration:0.5 μM; 1 μM; 5 μM; 10 μM
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Incubation Time:24 h
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Result:Induced ERα degradation in LCC2 tamoxifen-resistant breast cancer cells in a concentration-dependent manner.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude mice[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.p.; once every 2 days
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Result:Exhibited significant tumor growth inhibition compared to vehicle control at all tested doses.
Demonstrated the highest efficacy at 10 mg/kg.
Caused no significant changes in animal mortality or body weight.
Showed no meaningful histopathological differences in heart, liver, or kidney tissue between treatment groups and controls, indicating low toxicity to normal tissues.
Chemical Information
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CAS No. 2775441-10-4
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Molecular Weight 568.57
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Formula C28H23F3N4O4S
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SMILES
O=S([C@@H]1[C@H]2C(C3=CC=C(N4C=NC=N4)C=C3)=C(C5=CC=C(O)C=C5)[C@H](O2)C1)(N(CC(F)(F)F)C6=CC=CC=C6)=O
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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 6 Related Classifications
HY-149081 Related Classifications
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Keywords
- ERα degrader 6
- 2775441-10-4
- ERα degrader6
- ERα degrader-6
- Estrogen Receptor/ERR
- Cytochrome P450
- endocrine-resistant breast cancer
- LCC2 breast cancer cells
- HEK293T cells
- Balb/c nude mice
- MCF-10A breast cells
- ESR1
- proteasome pathway
- estrogen receptor α
- MCF-7 ER+ breast cancer cells
- aromatase inhibitor
- Inhibitor
- inhibitor
- inhibit