2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Estrogen Receptor/ERR
  4. 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.

PROTAC ER Degrader-16

PROTAC ER Degrader-16 Chemical Structure

CAS No. : 2847829-86-9

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PROTAC ER Degrader-16 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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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)

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.

PROTAC ER Degrader-16 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-t Cmax Tmax T1/2 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 ESR1Y537S 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.
Molecular Weight

795.77

Formula

C47H54BN5O6
CAS No.
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
References
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PROTAC ER Degrader-16 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC ER Degrader-162847829-86-9PROTAC ER Degrader16PROTAC ER Degrader 16PROTACsEstrogen Receptor/ERRbreast cancerCAMA-1 human breast cancer cellsMCF-10A human breast epithelial cellsNOD/SCID miceCRBN E3 ligaseESR1 Y537S mutantERαT47d-kb-Luc human breast cancer cellsSprague Dawley ratsMCF-7 human breast cancer cellsInhibitorinhibitorinhibit

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PROTAC ER Degrader-16
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HY-183804
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