2. PROTAC Vitamin D Related/Nuclear Receptor
  3. PROTACs Androgen Receptor
  4. ARD-69

ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC).
ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

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

ARD-69

ARD-69 Chemical Structure

CAS No. : 2316837-10-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

ARD-69 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC)[1][2][3].
ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

IC50 & Target

VHL

 

Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
183 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay
Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay
[PMID: 30629437]
LNCaP IC50
0.25 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
[PMID: 30629437]
VCaP IC50
0.34 nM
Compound: 34; ARD-69
Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay
[PMID: 30629437]
In Vitro

ARD-69 (0.01-10 μM; 6-24 h) induces degradation of androgen receptor (AR) in LNCaP, VCaP and 22Rv1 prostate cancer cells in a dose- and time-dependent manner, with DC50 values ??of 0.86 nM, 0.76 nM and 10.4 nM, respectively, and the highest degradation rate is >95%[1].
ARD-69 (0.01-1000 nM; 7 d) significantly inhibits the proliferation of LNCaP, VCaP and 22Rv1 cells, with IC50 values ??of 0.25 nM, 0.34 nM and 183 nM, respectively[1].

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

ARD-69 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP, VCaP, 22Rv1 prostate cancer cells
Concentration: 0.01-1000 nM
Incubation Time: 7 days
Result: Inhibited cell growth with IC50s of 0.25 nM (LNCaP), 0.34 nM (VCaP), and 183 nM (22Rv1), significantly more effective (>100-fold) than AR antagonists like enzalutamide. qPCR analysis revealed dose-dependent suppression of AR-regulated genes (PSA, TMPRSS2, FKBP5) by >50% at 10 nM, while WB confirmed reduced AR protein levels correlating with growth inhibition.
In Vivo

ARD-69 (50 mg/kg; intraperitoneal injection; single dose) significantly reduces AR and PSA protein levels in tumor tissues in a VCaP xenograft tumor model in severe combined immunodeficient (SCID) mice, with the effect lasting for at least 48 hours[1].

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

Animal Model: Female severe combined immunodeficient (SCID) mice with VCaP xenograft tumors[1]
Dosage: 50 mg/kg, dissolved in an appropriate solvent (e.g., DMSO/saline formulation)
Administration: Intraperitoneal (IP) injection, single dose
Result: Significantly reduced androgen receptor (AR) and prostate-specific antigen (PSA) protein levels in tumor tissues, with effects detectable as early as 3 hours post-treatment and persisting for at least 48 hours.
Dose-dependently decreased in AR and PSA expression relative to the loading control GAPDH, indicating sustained pharmacodynamic activity in vivo.
Molecular Weight

1129.82

Formula

C62H74ClFN8O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(C#CC4CCN(C5CCN(C(C[C@H](NC([C@H]6N(C([C@@H](NC(C7(CC7)F)=O)C(C)(C)C)=O)C[C@H](O)C6)=O)C8=CC=C(C9=C(C)N=CS9)C=C8)=O)CC5)CC4)C=C3)=O)C2(C)C)=CC=C1C#N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (44.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8851 mL 4.4255 mL 8.8510 mL
5 mM 0.1770 mL 0.8851 mL 1.7702 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 (protect from light, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 1.25 mg/mL (1.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (protect from light, 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 0.8851 mL 4.4255 mL 8.8510 mL 22.1274 mL
5 mM 0.1770 mL 0.8851 mL 1.7702 mL 4.4255 mL
10 mM 0.0885 mL 0.4425 mL 0.8851 mL 2.2127 mL
15 mM 0.0590 mL 0.2950 mL 0.5901 mL 1.4752 mL
20 mM 0.0443 mL 0.2213 mL 0.4425 mL 1.1064 mL
25 mM 0.0354 mL 0.1770 mL 0.3540 mL 0.8851 mL
30 mM 0.0295 mL 0.1475 mL 0.2950 mL 0.7376 mL
40 mM 0.0221 mL 0.1106 mL 0.2213 mL 0.5532 mL
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ARD-69 Related Classifications

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:

ARD-692316837-10-0ARD69ARD 69PROTACsAndrogen ReceptorAR-positive prostate cancer cell linesgene expressionInhibitorinhibitorinhibit

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