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Cat. No.: HY-183804

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PROTAC ER Degrader-16

PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC₅₀ of 1.4 nM and an IC₅₀ of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research.
(Pink: ERα ligand (HY-184091); Blue: Cereblon ligand (HY-132226); Black: linker).

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

CAS No.: 2847829-86-9
Formula: C₄₇H₅₄BN₅O₆
Molecular Weight:795.77

Storage:

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

PROTAC ER Degrader-16 Chemical Structure

CAS No.: 2847829-86-9

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Use of MCE Products

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

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

Biological Activity

Description

PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC₅₀ of 1.4 nM and an IC₅₀ of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research^[1]. (Pink: ERα ligand (HY-184091); Blue: Cereblon ligand (HY-132226); Black: linker).

IC₅₀ & Target^[1]

ERα

1.4 nM (DC₅₀)

ERα

1.9 nM (IC₅₀)

All PROTACs Isoforms :

All Estrogen Receptor/ERR Isoforms :

In Vitro

PROTAC ER Degrader-16 (Compound 4r) potently inhibits the transcriptional activity of estrogen receptor in T47d-kb-Luc human breast cancer cells, with an IC₅₀ value of 1.9 nM^[1].
PROTAC ER Degrader-16 (5 days) potently degrades estrogen receptor α protein in MCF-7 human breast cancer cells, with a DC₅₀ of 1.4 nM^[1].
PROTAC ER Degrader-16 (3 days) potently inhibits the proliferation of human breast cancer MCF-7 cells, with an IC₅₀ value of 2.3 nM^[1].
PROTAC ER Degrader-16 degrades estrogen receptor α protein in human breast cancer cell line CAMA-1^[1].
PROTAC ER Degrader-16 exhibits low cytotoxicity in non-tumorigenic human mammary epithelial cells MCF-10A, with only minimal reduction in cell viability even at high concentrations^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_0-t	C_max	T_max	T_1/2	Bioavailability
Rat^[1]	1.0 mg/kg	i.v.	1943 ng·h/mL	/	/	/	/
Rat^[1]	10 mg/kg	p.o.	6102 ng·h/mL	523 ng/mL	4.0 h	6.5 h	31.4 %

In Vivo

PROTAC ER Degrader-16 (Compound 4r) (20 mg/kg; p.o.; once daily; for 25 days) inhibits the growth of MCF-7 breast cancer xenografts in female NOD/SCID mice^[1].
PROTAC ER Degrader-16 (20 mg/kg; p.o.; once daily; for 40 consecutive days) inhibits the growth of ST1799 breast cancer PDX tumors, and its combination with Abemaciclib (HY-16297A) achieves complete tumor regression in immunodeficient mice^[1].
PROTAC ER Degrader-16 (20 mg/kg; p.o.; daily administration for 40 consecutive days) exerts potent tumor growth inhibitory effects in the tamoxifen (HY-13757A)-resistant ESR1^Y537S mutant ST941 breast cancer PDX model^[1].

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

Animal Model:

NOD/SCID (female, 6-8 weeks of age)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 25 days
Result:

Showed superior efficacy in blocking tumor growth compared to fulvestrant.
Was well tolerated with minimal body weight changes relative to vehicle controls.

Animal Model:

Immune-deficient^[1]
Dosage:

20 mg/kg (monotherapy); 20 mg/kg (combination with abemaciclib)
Administration:

p.o.; daily; 40 days
Result:

Inhibited ST1799 PDX tumor growth as monotherapy.
Achieved complete tumor regression in combination with abemaciclib.
Both treatments were well tolerated with minimal body weight changes relative to vehicle controls.

Animal Model:

Immune-deficient^[1]
Dosage:

20 mg/kg (monotherapy); 20 mg/kg (combination with palbociclib 50 mg/kg)
Administration:

p.o.; daily; 40 days
Result:

Inhibited ST941 PDX tumor growth more effectively than fulvestrant as monotherapy.
Enhanced efficacy in blocking tumor growth when combined with palbociclib.
All treatments were well tolerated with minimal body weight changes relative to vehicle controls.

Chemical Information

CAS No. 2847829-86-9
Molecular Weight 795.77
Formula C₄₇H₅₄BN₅O₆
SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)B(O)O)/C3=CC=C(C=C3)OCCN4CCN(CC4)CC5CCN(CC5)C6=CC7=C(C(N(C7)C8CCC(NC8=O)=O)=O)C=C6
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

Handling Instructions (2659 KB)

References

[1]. Peng X, et al. Developing orally active estrogen receptor degraders by conjugation of boronic tamoxifen and cereblon ligands. Eur J Med Chem. 2026;315:118956. [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
Purity & Documentation
References

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PROTAC ER Degrader-16

All PROTACs Isoforms

All Estrogen Receptor/ERR Isoforms