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  3. ERα degrader 4

ERα degrader 4 

Cat. No.: HY-144306
Handling Instructions

ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the treatment of breast cancer.

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

ERα degrader 4 Chemical Structure

ERα degrader 4 Chemical Structure

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Description

ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the treatment of breast cancer[1].

IC50 & Target

IC50: 0.31 μM (ERα) in MDA-MB-231, 0.41 μM (ERα) in MCF-7, 0.48 μM (ERα) in MCF-7/ADR[1]

In Vitro

ERα degrader 4 (compound 16a) (0-10 μM; 48 hours) has the high activity (IC50: 0.31-0.48 μM) against all tested cancer cell lines[1].
ERα degrader 4 (1 μM; 24 hours) increases ERα degradation and relative binding affinity in MCF-7 cancer cells[1].
ERα degrader 4 (0.5, 1 and 2 μM; 24 hours) decreases the number and size of MCF-7 cells colonies at 0.5 μM, and completely suppresses colony formation with 2 μM[1].
ERα degrader 4 (0.5, 1, 2 μM; 24 hours) increases the early-stage apoptosis of MCF-7 cells with a dose-dependent manner[1].
ERα degrader 4 (0.5, 1, 2 μM; 24 hours) can induce the accumulation of reactive oxygen species (ROS) which contributes to the apoptosis of MCF-7 cells[1].
ERα degrader 4 (0.5, 1, 2 μM; 24 hours) induces apoptosis in MCF-7 cancer cells by decreasing the mitochondrial membrane potential[1].

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

Cell Cytotoxicity Assay

Cell Line: MDA-MB-231, MCF-7, MCF-7/ADR and MCF-10A cells[1]
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Showed the high activity (IC50: 0.31-0.48 μM) against all tested cancer cell lines.

Cell Cycle Analysis

Cell Line: MCF-7 cells[1]
Concentration: 0.5, 1, 2 and 3 μM
Incubation Time: 24 hours
Result: Induced cell cycle arrest at G1 phase.

Apoptosis Analysis

Cell Line: MCF-7 cells[1]
Concentration: 0.5, 1 and 2 μM
Incubation Time: 24 hours
Result: Increased the early-stage apoptosis of MCF-7 cells with a dose-dependent manner.
Molecular Weight

690.91

Formula

C42H58O8

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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ERα degrader 4
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HY-144306
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