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

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 research of breast cancer.

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ERα degrader 4

ERα degrader 4 Chemical Structure

CAS No. : 2763464-53-3

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ERα degrader 4 Related Antibodies

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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 research 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]
Cellular Effect
Cell Line Type Value Description References
MCF-10A IC50
2.19 μM
Compound: 16a
Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 34992039]
MCF7 IC50
0.41 μM
Compound: 16a
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 34992039]
MCF7 IC50
0.41 μM
Compound: 16a; 24
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
[PMID: 37607438]
MCF7 IC50
0.41 μM
Compound: 86
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
[PMID: 36205223]
MCF7 IC50
0.48 μM
Compound: 16a
Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 34992039]
MDA-MB-231 IC50
0.31 μM
Compound: 16a
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 34992039]
MDA-MB-231 IC50
0.31 μM
Compound: 16a; 24
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 37607438]
NCI/ADR-RES IC50
0.48 μM
Compound: 16a; 24
Antiproliferative activity against human MCF7ADR cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7ADR cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
[PMID: 37607438]
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].

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

ERα degrader 4 Related Antibodies

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
CAS No.
SMILES

[H][C@]12C[C@]3(CC[C@]([C@H](/C=C\C=C/C(OCCOCCOCCOC(CC45CC6CC(C5)CC(C6)C4)=O)=O)C)([C@@]3(C/C=C([C@@]1(C(C=C2C)=O)[H])/C=O)[H])[H])C
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 4 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 42763464-53-3ERα degrader4ERα degrader-4Estrogen Receptor/ERRApoptosisSERDERαG1 phaseBreast cancerMCF-7?cellsSelectiveInhibitorinhibitorinhibit

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