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Cat. No.: HY-132194

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ERα degrader-2

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Based on 1 Customer Validation

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC₅₀=17.1 nM), good degradation efficacy (EC₅₀=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER⁺ breast cancer research.

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

Purity: 98.30%
CAS No.: 2235396-63-9
Formula: C₂₉H₂₇F₃N₂O₂
Molecular Weight:492.53

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ERα degrader-2 Chemical Structure

CAS No.: 2235396-63-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

ERα

4.6 nM (IC₅₀)

All Estrogen Receptor/ERR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
ES-2	IC₅₀	17.1 nM Compound: D24	Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay	[PMID: 34056898]
MCF7	IC₅₀	0.27 nM Compound: D24	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay	[PMID: 34056898]

In Vitro

ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells^[1].

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

In Vivo

ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice^[1].
ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%^[1].

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

Animal Model:

MCF-7 human breast cancer xenograft model in nude mice^[1]
Dosage:

2 mg/kg; 6 mg/kg
Administration:

Oral administration; 2-6 mg/kg; QD; 21 days
Result:

Exhibited in vivo efficacy in breast cancer xenograft model.

Chemical Information

CAS No. 2235396-63-9
Appearance Solid
Molecular Weight 492.53
Formula C₂₉H₂₇F₃N₂O₂
Color Brown to reddish brown
SMILES

CC(C)(F)CN1[C@@](C2=C(C=C(C3=CC=C(C=C3)C(O)=O)C=C2F)F)([H])C4=C(C[C@H]1C)C5=CC=CC=C5N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : < 1 mg/mL (insoluble or slightly soluble)

View the Complete Stock Solution Preparation Table

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Xiaomeng Zhang, et al. Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ERα+ Breast Cancer. J Med Chem [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.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References

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ERα degrader-2

MCE Bioactive Compound Library

All Estrogen Receptor/ERR Isoforms