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

ARD-266 

Cat. No.: HY-133020 Purity: 99.67%
Handling Instructions

ARD-266 is 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 Price Stock Quantity
5 mg USD 1850 In-stock
Estimated Time of Arrival: December 31
10 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

ARD-266 is 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].

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

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (109.23 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0923 mL 5.4614 mL 10.9229 mL
5 mM 0.2185 mL 1.0923 mL 2.1846 mL
10 mM 0.1092 mL 0.5461 mL 1.0923 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (5.46 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (5.46 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (5.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.67%

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Keywords:

ARD-266ARD266ARD 266PROTACAndrogen ReceptorProteolysis-targeting chimeraInhibitorinhibitorinhibit

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Product Name:
ARD-266
Cat. No.:
HY-133020
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