1. PROTAC Vitamin D Related/Nuclear Receptor
  2. PROTACs Estrogen Receptor/ERR
  3. PROTAC ER Degrader-4

PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.

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

PROTAC ER Degrader-4 Chemical Structure

PROTAC ER Degrader-4 Chemical Structure

CAS No. : 2361114-15-8

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1 mg USD 356 In-stock
5 mg USD 890 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM[1].

IC50 & Target[1]

VHL

 

ER

 

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
0.3 nM
Compound: Ex 3
Induction of VHL E3 ligase mediated ERalpha degradation in human MCF7 cells assessed as downregulation of ERalpha expression by cell-based immunofluorescence assay
Induction of VHL E3 ligase mediated ERalpha degradation in human MCF7 cells assessed as downregulation of ERalpha expression by cell-based immunofluorescence assay
[PMID: 31620216]
In Vitro

PROTAC ER Degrader-4 shows equal to 100% ER degradation at 0.3 μM in the MCF-7 ER degradation cellular assay[1].

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

Molecular Weight

1005.19

Formula

C53H67F3N6O8S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(F)CN1[C@H](C2=C(C=C(OCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@@H](O)C3)C(N[C@H](C4=CC=C(C5=C(N=CS5)C)C=C4)C)=O)=O)=O)C=C2F)F)C6=C(C7=CC=CC=C7N6)C[C@H]1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (99.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9948 mL 4.9742 mL 9.9484 mL
5 mM 0.1990 mL 0.9948 mL 1.9897 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9948 mL 4.9742 mL 9.9484 mL 24.8709 mL
5 mM 0.1990 mL 0.9948 mL 1.9897 mL 4.9742 mL
10 mM 0.0995 mL 0.4974 mL 0.9948 mL 2.4871 mL
15 mM 0.0663 mL 0.3316 mL 0.6632 mL 1.6581 mL
20 mM 0.0497 mL 0.2487 mL 0.4974 mL 1.2435 mL
25 mM 0.0398 mL 0.1990 mL 0.3979 mL 0.9948 mL
30 mM 0.0332 mL 0.1658 mL 0.3316 mL 0.8290 mL
40 mM 0.0249 mL 0.1244 mL 0.2487 mL 0.6218 mL
50 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4974 mL
60 mM 0.0166 mL 0.0829 mL 0.1658 mL 0.4145 mL
80 mM 0.0124 mL 0.0622 mL 0.1244 mL 0.3109 mL
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  • 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.

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Product Name:
PROTAC ER Degrader-4
Cat. No.:
HY-135309
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