country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-174453

Copy Link Print Information

PROTAC ERα Degrader-12

PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer.
(Pink: ERα ligand (HY-174475); Blue: VHL ligand (HY-112078); Black: linker (HY-W088749)).

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

Formula: C₅₃H₈₃N₇O₅S
Molecular Weight:930.34

Storage:

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

Data Sheet (278 KB)

PROTAC ERα Degrader-12 Chemical Structure

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer^[1]. (Pink: ERα ligand (HY-174475); Blue: VHL ligand (HY-112078); Black: linker (HY-W088749)).

IC₅₀ & Target^[1]

ERα

VHL

All PROTACs Isoforms :

All Estrogen Receptor/ERR Isoforms :

In Vitro

PROTAC ERα Degrader-12 (Compound CP03) (0.1-10 μM, 24 h) demonstrates significant ERα degradation activity in MCF-7 cells with DC₅₀ value of 1.02 μM^[1].
PROTAC ERα Degrader-12 (0.01-100 μM, 24 h) exhibits potent anticancer activity in MCF-7 cells (IC₅₀ = 0.17 μM)^[1].
PROTAC ERα Degrader-12 exhibits remarkable stability in human liver microsomes and plasma with the level of plasma protein binding of 97.8%^[1].
PROTAC ERα Degrader-12 (1-5 μM, 48 h) halts the cell cycle progression in the G1 phase and induces substantial cellular death and damage in MCF-7^[1].

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

Western Blot Analysis^[1]

Cell Line:

MCF-7, MDA-MB-321, MCF-7^Y537S, MCF-7^D538G, MCF-7^EGFR, and LCC-2 cell lines
Concentration:

0.1, 0.2, 1, 2, 5, 10 μM
Incubation Time:

24 h
Result:

Effectively induced ERα degradation in a dose-dependent manner in MCF-7 cells.
Efficiently reduced the Erα^MUT levels in both the MCF-7^Y537S and MCF-7^D538G cell lines with DC₅₀ values of 0.83 and 0.55 μM, respectively.
Showed high degradation potency for ERα in MCF-7^EGFR and LCC-2 cell lines, with DC₅₀ values of 0.13 and 1.40 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

MCF-7
Concentration:

2 μM
Incubation Time:

24 h
Result:

Was markedly suppressed in the presence of CoA-1 or CoA-2.

Cell Viability Assay^[1]

Cell Line:

MCF-7, MDA-MB-321, MCF-7^Y537S, MCF-7^D538G, MCF-7^EGFR, and LCC-2 cell lines
Concentration:

0.01, 0.1, 1, 10, 100 μM
Incubation Time:

24 h
Result:

Had no notable inhibitory influence on cell growth in the ER-negative cell line MDA-MB-231 at concentrations exceeding 100 μM.
Exhibited excellent antiproliferative activity in MCF-7^Y537S, MCF-7^D538G, and MCF-7^EGFR, with IC₅₀ values that were 10.3-, 19.4-, and 58.0-fold higher than those of Ful, respectively.
Displayed enhanced antiproliferative efficacy against Tamoxifen (HY-13757A)-resistant LCC-2 cells, with an IC₅₀ value that was 8.04-fold higher than that of Fulvestrant (HY-13636).

RT-PCR^[1]

Cell Line:

MCF-7
Concentration:

0.1, 1 μM
Incubation Time:

24 h
Result:

Had no discernible impact on the mRNA of ERα expression.

Apoptosis Analysis^[1]

Cell Line:

MCF-7, MDA-MB-321, MCF-7^Y537S, MCF-7^D538G, MCF-7^EGFR, and LCC-2 cell lines
Concentration:

1, 5 μM
Incubation Time:

48 h
Result:

Induced substantial cellular death and damage in a concentration-dependent manner.
Effectively halted the cell cycle progression in the G1 phase.

In Vivo

PROTAC ERα Degrader-12 (Compound CP03) (1-4 mg/kg, i.p., every other day for 26 or 33 days) exhibits significant tumor-inhibitory effects in mice MCF-7 and LCC-2 tumor xenograft models^[1].

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

Animal Model:

MCF-7 and LCC-2 tumor xenograft models established in female BALB/c nude mice (15-18 g, 5 weeks old) ^[1]
Dosage:

1, 2, 4 mg/kg
Administration:

Intraperitoneal injection (i.p.), every other day, for 26 or 33 days.
Result:

Showed significant tumor growth inhibitory activity at 2 mg/kg.
Had no significant host toxicity as monitored by changes in the body weight.
Almost completely inhibited tumor growth on day 33 at a dose of 2 or 4 mg/kg.
Effectively induced significant degradation of ERα with 2 mg/kg.

Chemical Information

Molecular Weight 930.34
Formula C₅₃H₈₃N₇O₅S
SMILES

CC(C)([C@H](NC(CCCCC(NCC1=C(C(CN)=C(C(CN)=C1CCCCC)CCCCC)CCCCC)=O)=O)C(N2C[C@H](O)C[C@H]2C(N[C@H](C3=CC=C(C=C3)C4=C(C)N=CS4)C)=O)=O)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 (278 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]. Wang Y, et al. Targeted Degradation of the Estrogen Receptor α through Unconventional Coactivator Binding Site (CBS). J Med Chem. 2025 Jul 10;68(13):13640-13660. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

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

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PROTAC ERα Degrader-12

All PROTACs Isoforms

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC ERα Degrader-12 Related Classifications

HY-174453 Related Classifications