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

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

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

PROTAC ERα Degrader-4 Chemical Structure

PROTAC ERα Degrader-4 Chemical Structure

CAS No. : 2521299-80-7

Size Price Stock
1 mg USD 540 Ask For Quote & Lead Time
5 mg USD 1350 Ask For Quote & Lead Time
10 mg USD 2200 Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PROTAC ERα Degrader-4 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC ERα Degrader-4 is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.

IC50 & Target[1]

ERα

5.08 μM (Ki)

ERβ

26.20 μM (Ki)

In Vitro

PROTAC ERα Degrader-4 (1 μM, 12 hours) exhibits significant degradation activity for ERα in MCF-7cells[1].
PROTAC ERα Degrader-4 (2 μM, 12 hours) can degrade wild-type ERα inT47D cells and mutant ERα in T47DD538G and T47DY537S cells[1].
PROTAC ERα Degrader-4 (0.01-10 μM, 72 hours) has inhibitory activity of ERα in Tamoxifen (HY-13757A) -sensitive MCF-7 cells, with the IC50 value of 0.05 μM[1].
PROTAC ERα Degrader-4 (1-10 μM, 72 hours) induce apoptosis and cell cycle arrest of MCF-7 cells[1].
PROTAC ERα Degrader-4 (0.01-10 μM, 12 hours) efficiently degrades ERα protein in the range of 0.01 to10 μM in MCF-7 cell line[1].

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

PROTAC ERα Degrader-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Had inhibitory activity in Tamoxifen-sensitive MCF-7 cells, with the IC50 value of 0.05 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.0 μM, 5 μM, 5.0 μM
Incubation Time: 72 hours
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 72 hours
Result: Induced cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01-10 μM
Incubation Time: 12 hours
Result: Efficiently degraded ERα protein in the range of 0.01 to10 μM, whereas ERα protein levels recovered slightly at a high concentration of 10 μM
In Vivo

PROTAC ERα Degrader-4 (Compound ZD12) (5 μM/kg for i.p., once every 2 days) exhibits potent antitumor activity and ERα degradation effect in tumor tissues in LCC2 orthotopic xenograft tumor models[1].
PROTAC ERα Degrader-4 (5 mg/kg for i.v.) shows a T1/2 of 4.61 h and CL of 64.4 mL/min/kg[1].

Pharmacokinetic parameters for PROTAC ERα Degrader-4 (Compound ZD12) in BALB/C female mice[1]

ND: not detected.
Route Dose (mg/kg) CL (mL/min/kg) Tmax (h) T1/2 (h) Cmax (ng/mL) AUC (h•ng/mL)
i.v. 5 64.4 0.08 4.61 3635.73 1342
p.o. 20 ND ND ND ND ND

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

Animal Model: LCC2 orthotopic xenograft tumor models[1]
Dosage: 5 μM/kg
Administration: Intravenous injection (i.p.)
Result: Exhibited potent antitumor activity and ERα degradation effect in tumor tissues.
Animal Model: BALB/C female mice (Pharmacokinetic assay)[1]
Dosage: 5 mg/kg; 20 mg/kg
Administration: Intravenous injection (i.v.); Oral gavage (p.o.)
Result:
Molecular Weight

1074.23

Formula

C55H62F3N5O10S2
CAS No.
SMILES

CC1=C(C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@@H](NC(CCCCCOC4=CC=C(C=C4)N(CC(F)(F)F)S(C5C[C@@H]6C(C7=CC=C(C=C7)O)=C([C@H]5O6)C8=CC=C(C=C8)O)(=O)=O)=O)C(C)(C)C)=O)O)=O)C)SC=N1
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC ERα Degrader-4 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 ERα Degrader-42521299-80-7PROTAC ERα Degrader4PROTAC ERα Degrader 4PROTACsEstrogen Receptor/ERRApoptosisPROTAC ERα DegraderMCF-7primary astrocytesER-positive breast cancerxenograft tumor modelsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC ERα Degrader-4
Cat. No.:
HY-149295
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.