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Cat. No.: HY-144306

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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.

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

CAS No.: 2763464-53-3
Formula: C₄₂H₅₈O₈
Molecular Weight:690.91

Storage:

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

Data Sheet (269 KB)

ERα degrader 4 Chemical Structure

CAS No.: 2763464-53-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

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]

All Estrogen Receptor/ERR Isoforms :

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.

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.

Chemical Information

CAS No. 2763464-53-3
Molecular Weight 690.91
Formula C₄₂H₅₈O₈
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Liang JJ, et al. Design and synthesis of marine sesterterpene analogues as novel estrogen receptor α degraders for breast cancer treatment. Eur J Med Chem. 2022;229:114081. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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