Art. -Nr.: HY-174453

PROTAC ERα Degrader-12

PROTAC ERα Degrader-12 is a VHL-recruiting ERα PROTAC degrader with a DC₅₀ of 1.02 μM in MCF-7 cells. PROTAC ERα Degrader-12 binds to ERα and recruits the VHL E3 ligase to form a ternary complex, promoting proteasomal degradation of both wild-type and mutant ERα, thereby inhibiting ER-mediated transcriptional activity and breast cancer cell proliferation. PROTAC ERα Degrader-12 can be used in the research of ERα-positive breast cancer.
(Pink: ERα ligand (HY-174475); Blue: VHL ligand (HY-112078); Black: linker (HY-W088749)).

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Formel: C₅₃H₈₃N₇O₅S
Molecular Weight:930.34

Speicherung:

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

Data Sheet (292 KB)

PROTAC ERα Degrader-12 Chemical Structure

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC ERα Degrader-12 is a VHL-recruiting ERα PROTAC degrader with a DC₅₀ of 1.02 μM in MCF-7 cells. PROTAC ERα Degrader-12 binds to ERα and recruits the VHL E3 ligase to form a ternary complex, promoting proteasomal degradation of both wild-type and mutant ERα, thereby inhibiting ER-mediated transcriptional activity and breast cancer cell proliferation. PROTAC ERα Degrader-12 can be used in the research of ERα-positive breast cancer^[1]. (Pink: ERα ligand (HY-174475); Blue: VHL ligand (HY-112078); Black: linker (HY-W088749)).

IC₅₀ & Target

^[1]

ERα

1.02 μM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	DC₅₀	1.02 μM	Induction of wild-type ERα degradation in human MCF-7 breast cancer cells incubated for 24 hrs, measured via Western blot assay. Induction of wild-type ERα degradation in human MCF-7 breast cancer cells incubated for 24 hrs, measured via Western blot assay.	40527751
MCF7	DC₅₀	0.13 μM	Induction of ERα degradation in human MCF-7^EGFR EGFR-overexpressing/ERα-positive breast cancer cells incubated for 24 hrs, measured via Western blot assay. Induction of ERα degradation in human MCF-7^EGFR EGFR-overexpressing/ERα-positive breast cancer cells incubated for 24 hrs, measured via Western blot assay.	40527751
MCF7	IC₅₀	0.17 μM	Antiproliferative activity against human MCF-7 wild-type ERα breast cancer cells. Antiproliferative activity against human MCF-7 wild-type ERα breast cancer cells.	40527751
MCF7	IC₅₀	0.02 μM	Antiproliferative activity against human MCF-7^EGFR EGFR-overexpressing/ERα-positive breast cancer cells. Antiproliferative activity against human MCF-7^EGFR EGFR-overexpressing/ERα-positive breast cancer cells.	40527751

In Vitro

PROTAC ERα Degrader-12 (compound CP03) (0.1-10 μM; 24 h) induces dose-dependent degradation of wild-type ERα in MCF-7 cells, with a DC₅₀ of 1.02 μM after 24 h of incubation^[1].
PROTAC ERα Degrader-12 (0.1-10 μM; 24 h) induces dose-dependent degradation of the ERα^Y537S mutant in MCF-7^Y537S cells, with a DC₅₀ of 0.83 μM after 24 h of incubation^[1].
PROTAC ERα Degrader-12 (0.1-10 μM; 24 h) induces dose-dependent degradation of D538G-mutant ERα in MCF-7^D538G cells, with a DC₅₀ of 0.55 μM after 24 h of incubation^[1].
PROTAC ERα Degrader-12 (0.1-10 μM; 24 h) induces dose-dependent degradation of ERα in MCF-7^EGFR cells, with a DC₅₀ of 0.13 μM after 24 h of incubation^[1].
PROTAC ERα Degrader-12 (0.1-10 μM; 24 h) induces dose-dependent degradation of ERα in Tamoxifen (HY-13757A)-resistant LCC-2 cells, with a DC₅₀ of 1.40 μM after 24 h of incubation^[1].
PROTAC ERα Degrader-12 (2 μM; 24 h)-induced ERα degradation in MCF-7, MCF-7^Y537S, MCF-7^D538G, MCF-7^EGFR and LCC-2 cells depends on the proteasome pathway^[1].
PROTAC ERα Degrader-12 potently inhibits the proliferation of MCF-7^Y537S cells, with an IC₅₀ of 0.11 μM^[1].
PROTAC ERα Degrader-12 potently inhibits the proliferation of MCF-7^D538G cells, with an IC₅₀ value of 0.06 μM^[1].
PROTAC ERα Degrader-12 potently inhibits the proliferation of MCF-7^EGFR cells, with an IC₅₀ value of 0.02 μM^[1].
PROTAC ERα Degrader-12 inhibits the proliferation of tamoxifen-resistant LCC-2 cells, with an IC₅₀ value of 1.43 μM^[1].
PROTAC ERα Degrader-12 potently inhibits E₂-induced ER-responsive transcriptional activity in MCF-7 cells^[1].
PROTAC ERα Degrader-12 inhibits the protein-protein interaction between ERα and coactivators at CBS with an IC₅₀ value of 3.70 μM in cell-free TR-FRET assays^[1].
PROTAC ERα Degrader-12 binds to ERα^Y537S with a binary dissociation constant K_D of 1.38 μM; in cell-free SPR assays, it also forms a stable ternary complex with ERα^Y537S and VHL, with a ternary dissociation constant K_D of 0.14 μM^[1].
PROTAC ERα Degrader-12 (2 μM; 24 h) induces ERα degradation in MCF-7 cells in a coactivator binding site (CBS)-dependent manner^[1].
PROTAC ERα Degrader-12 (5 μM; 24 h) does not degrade ERβ in ERβ-overexpressing H1975 cells^[1].
PROTAC ERα Degrader-12 (2-5 μM; 24 h) does not degrade androgen receptor (AR) in MCF-7, MCF-7^Y537S, MCF-7^D538G, MCF-7^EGFR or LCC-2 cells^[1].
PROTAC ERα Degrader-12 potently inhibits the proliferation of MCF-7 cells, with an IC₅₀ of 0.17 μM and a selectivity index of 154.5^[1].
PROTAC ERα Degrader-12 (24 h) does not alter the mRNA expression of ERα in MCF-7 cells^[1].
PROTAC ERα Degrader-12 (1.5 μM) exhibits high stability in human liver microsomes, with a half-life > 60 min^[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 wild-type ERα breast cancer cells
Concentration:

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

24 h
Result:

Induced dose-dependent degradation of wild-type ERα, with a half-maximal degradation concentration (DC₅₀) of 1.02 μM.

Western Blot Analysis^[1]

Cell Line:

MCF-7^Y537S mutant ERα breast cancer cells
Concentration:

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

24 h
Result:

Induced dose-dependent degradation of Y537S mutant ERα, with a half-maximal degradation concentration (DC₅₀) of 0.83 μM.

Western Blot Analysis^[1]

Cell Line:

MCF-7^D538G mutant ERα breast cancer cells
Concentration:

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

24 h
Result:

Induced dose-dependent degradation of D538G mutant ERα, with a half-maximal degradation concentration (DC₅₀) of 0.55 μM.

Western Blot Analysis^[1]

Cell Line:

MCF-7^EGFR EGFR-overexpressing/ERα-positive breast cancer cells
Concentration:

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

24 h
Result:

Induced dose-dependent degradation of ERα, with a half-maximal degradation concentration (DC₅₀) of 0.13 μM.

Western Blot Analysis^[1]

Cell Line:

LCC-2 tamoxifen-resistant ERα-positive breast cancer cells
Concentration:

0.1-10 μM
Incubation Time:

24 h
Result:

Induced dose-dependent degradation of ERα, with a half-maximal degradation concentration (DC₅₀) of 1.40 μM.

Western Blot Analysis^[1]

Cell Line:

H1975 ERβ-overexpressing cells
Concentration:

5 μM
Incubation Time:

24 h
Result:

Did not induce degradation of ERβ protein in H1975 cells.

Western Blot Analysis^[1]

Cell Line:

MCF-7, MCF-7^Y537S, MCF-7^D538G, MCF-7^EGFR, and LCC-2 breast cancer cells
Concentration:

2, 5 μM
Incubation Time:

24 h
Result:

Did not induce degradation of AR protein in any of the tested cell lines.

In Vivo

PROTAC ERα Degrader-12 (compound CP03) (2-4 mg/kg; i.p.; every other day) almost completely inhibits MCF-7 breast cancer xenograft tumor growth and induces significant ERα degradation in vivo^[1].
PROTAC ERα Degrader-12 (2 mg/kg; i.p.; every other day) exhibits superior tumor growth inhibition compared to fulvestrant at the same dose and induces significant ERα degradation in Tamoxifen-resistant LCC-2 breast cancer xenografts in vivo^[1].

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

Animal Model:

BALB/c nude mice (female, 5 weeks old, 15-18 g, subcutaneous xenograft of MCF-7 cells)^[1]
Dosage:

1 mg/kg; 2 mg/kg; 4 mg/kg
Administration:

i.p.; every other day
Result:

Almost completely inhibited tumor growth at 2 mg/kg or 4 mg/kg, comparable to positive controls.
Induced significant degradation of ERα in MCF-7 xenograft tumors at 2 mg/kg.
Reduced the proportion of Ki67-positive tumor cells relative to the control group at 2 mg/kg.
Showed no significant host toxicity, as monitored by body weight changes and histology of heart, liver, and kidney tissues.

Animal Model:

BALB/c nude mice (female, 5 weeks old, 15-18 g, subcutaneous xenograft of tamoxifen-resistant LCC-2 cells)^[1]
Dosage:

2 mg/kg
Administration:

i.p.; every other day
Result:

Exhibited significant tumor growth inhibitory activity superior to fulvestrant at the same dose.
Induced significant degradation of ERα in LCC-2 xenograft tumors.
Reduced the proportion of Ki67-positive tumor cells relative to the control group.
Showed no significant host toxicity, as monitored by body weight changes and histology of heart, liver, and kidney tissues.

Chemical Information

Molecular Weight 930.34
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 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)

Verweise

[1]. Wang Y, et al. Targeted Degradation of the Estrogen Receptor α through Unconventional Coactivator Binding Site (CBS). Journal of medicinal chemistry. 2025 Jul 10;68(13):13640-13660. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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PROTAC ERα Degrader-12

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen