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

ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity.

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

ER degrader 4 Chemical Structure

ER degrader 4 Chemical Structure

CAS No. : 2913192-39-7

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Description

ER degrader 4 is a selective and orally active estrogen receptor degrader. ER degrader 4 has anti-tumor activity[1].

In Vitro

ER degrader 4 (Compound 22h) inhibits MCF-7 cell proliferation with an IC50 of 0.20 μM[1].
ER degrader 4 (1 nM-10 μM, 24 h) degrades ER in MCF-7 cells dose-dependently[1].
ER degrader 4 (10 μM, 24 h) decreases the gene expression levels of GREB1, PGR, and TFF1 in MCF-7 cells[1].
ER degrader 4 (10 μM, 24 h) arrests MCF-7 cells in G0/G1 phase[1].

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

Western Blot Analysis[7]

Cell Line: MCF-7 cell
Concentration: 1 nM, 100 nM, 1 μM and 10 μM
Incubation Time: 24 h
Result: Degraded ER dose-dependently, shows maximum degradation at 10 μM.
In Vivo

ER degrader 4 (Compound 22h) (30 mg/kg, oral gavage) inhibits tumor growth in a MCF-7 xenograft model[1].

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

Animal Model: MCF-7 xenograft model[3]
Dosage: 30 mg/kg
Administration: Oral gavage
Result: Significantly inhibited tumor growth with no significant body weight loss.
Reduces protein level of Ki67, ER, and PR in resected xenograft tumors.
Molecular Weight

446.49

Formula

C26H19FO4S

CAS No.
Unlabeled Cas

SMILES

O=C(C1=C(C=C(C=C1)C)C)C(SC2=CC(F)=CC=C23)=C3OC4=CC=C(C=C4)/C=C/C(O)=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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ER degrader 4 Related Classifications

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  • 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.

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Product Name:
ER degrader 4
Cat. No.:
HY-149969
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