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Art. -Nr.: 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).

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CAS. Nr.: 2847829-86-9
Formel: C₄₇H₅₄BN₅O₆
Molecular Weight:795.77

Speicherung:

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

PROTAC ER Degrader-16 Chemical Structure

CAS. Nr.: 2847829-86-9

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Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

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)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

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. Nr. 2847829-86-9
Molecular Weight 795.77
Formel 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
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

Handling Instructions (2659 KB)

Verweise

[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

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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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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PROTAC ER Degrader-16

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PROTAC ER Degrader-16 Related Classifications

HY-183804 Related Classifications