1. PROTAC
    Others
  2. PROTAC
    Androgen Receptor
  3. ARD-266

ARD-266 

Cat. No.: HY-133020
Handling Instructions

ARD-266 is a a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.

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

ARD-266 Chemical Structure

ARD-266 Chemical Structure

Size Stock
100 mg Get quote
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All PROTAC Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ARD-266 is a a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM[1].

IC50 & Target[1]

VHL

 

In Vitro

ARD-266 (Compound 11; 100 nM; 1-24 hours; LNCaP and VCaP cells) treatment effectively reduces the AR protein level within 3 h and achieves near-complete AR elimination with a 6 h treatment in the LNCaP cells[1].
ARD-266 (Compound 11; 1-10000 nM; 24 hours; LNCaP cells) treatment effectively suppresses the expression of PSA, TMPRSS2, and FKBP5 genes in a dosedependent manner and is capable of reducing the mRNA levels of PSA, TMPRSS2, and FKBP5 genes by >50% at 10 nM in the LNCaP cell line[1].

Western Blot Analysis[1]

Cell Line: LNCaP and VCaP cells
Concentration: 100 nM
Incubation Time: 1 hour, 3 hours, 6 hours, 12 hours, 24 hours
Result: Effectively reduced the AR protein level within 3 h and achieved near-complete AR elimination with a 6 h treatment in the LNCaP cells.

RT-PCR[1]

Cell Line: LNCaP cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 24 hours
Result: Effectively suppressed the expression of PSA, TMPRSS2, and FKBP5 genes in a dose-dependent manner and was capable of reducing the mRNA levels of PSA, TMPRSS2, and FKBP5 genes by >50% at 10 nM in the LNCaP cell line.
Molecular Weight

915.51

Formula

C₅₂H₅₉ClN₆O₇

SMILES

O=C(C[[email protected]@H](C1=CC=CC=C1)NC([[email protected]]2N(C([[email protected]](C(C)C)C3=CC(C)=NO3)=O)C[[email protected]](O)C2)=O)N(CC4)CCC4C#CC5=CC=C(C(N[[email protected]@H]6C(C)(C)[[email protected]@H](OC7=CC=C(C#N)C(Cl)=C7)C6(C)C)=O)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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.
  • 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

Keywords:

ARD-266ARD266ARD 266PROTACAndrogen ReceptorProteolysis-targeting chimeraPSATMPRSS2FKBP5VHLdegraderAR-positiveInhibitorinhibitorinhibit

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 *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
ARD-266
Cat. No.:
HY-133020
Quantity:
MCE Japan Authorized Agent: