2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  3. PROTACs Androgen Receptor Progesterone Receptor Apoptosis
  4. ARD-61

ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

ARD-61 Chemical Structure

ARD-61 Chemical Structure

CAS No. : 2316837-08-6

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1 mg USD 900 In-stock
5 mg USD 1980 In-stock
10 mg USD 3200 In-stock
25 mg USD 6400 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ARD-61 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1]. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

VHL

 

Cellular Effect
Cell Line Type Value Description References
LNCaP IC50
2 nM
Compound: 1; ARD-61
Antiproliferative activity against AR-positive human LNCAP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
Antiproliferative activity against AR-positive human LNCAP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
[PMID: 31804827]
VCaP IC50
2 nM
Compound: 1; ARD-61
Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay
[PMID: 31804827]
In Vitro

ARD-61 binds to AR protein through its AR antagonist portion and von Hippel-Lindau (VHL)/cullin 2 E3 ligase through its VHL ligand portion to recruit AR protein to cullin 2 for ubiquitination, followed by proteasome-dependent AR degradation[1].
ARD-61 (0.001-100 μM; for 7?days) has IC50 values of 235?nM and 121?nM in the MDA-MB-453 and HCC1428 cell lines, which have the highest AR expression, respectively. ARD-61 demonstrates partial cell growth inhibition, delivering IC50 values of 39, 147, and 380?nM, respectively, in the MCF-7, BT-549 and MDA-MB-415 cell lines, which have a moderate level of AR protein[1].
ARD-61 (25-100000 nM; 6-72 h) induces G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines[1].
ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 and HCC1428 cell lines[1].
ARD-61 (0.01-1000 nM; 6 h) is highly potent and effective in reducing AR protein levels. ARD-61 (0.01-1000 nM; 24 h) reduces the level of PR protein with a DC50 value of 0.15?nM in the T47D cells. ARD-61 has no obvious effect on ER and GR proteins[1].
ARD-61 (1?μM; for 24?h) effectively inhibits Wnt/β-catenin and MYC signaling pathways. ARD-61 (1-1000?nM; for 24?h) not only decreases both phosphorylated HER2 and HER3, but also un-phosphorylated HER2 and HER3 proteins[1].
Efficient knock-down of VHL completely blocks AR degradation induced by ARD-61 (100?nM; 24 h) in both MDA-MB-453 and MCF-7 cell lines[1].

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

ARD-61 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-453 and HCC1428 cell lines
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 7 days
Result: Achieves near complete inhibition of cell growth.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-453, HCC1428 and MCF-7 cell lines
Concentration: 25, 250, 500, 1000, 10000, 100000 nM
Incubation Time: 6-72 hours
Result: Induced G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines.

Apoptosis Analysis[1]

Cell Line: MDA-MB-453 and HCC1428 cell lines
Concentration: 25, 250, 500, 1000, 10000, 100000 nM
Incubation Time: 6-72 hours
Result: Induced apoptosis in the MDA-MB-453 and HCC1428 cell lines in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-453, MCF-7, BT549, MDA-MB-415 and HCC1428 cell lines
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 6 hours
Result: Reduced AR protein levels in the MDA-MB-453 (DC50=0.44 nM), MCF-7 (DC50=1.8 nM), BT549 (DC50=2.0 nM), MDA-MB-415 (DC50=2.4 nM) and HCC1428 (DC50=3.0 nM) cell lines.
In Vivo

ARD-61 (25, 50?mg/kg/day; ip; for 75 days) effectively inhibits tumor growthin the MDA-MB-453 xenograft tumor model in male SCID mice[1].
ARD-61 (25?mg/kg; ip; single dose) effectively and rapidly reduces the AR protein in the MDA-MB-453 xenograft tissue, with the effect persisting for at least 24?h. ARD-61 is very effective in reducing the mRNA level of WNT7B in a time-dependent manner[1].

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

Animal Model: MDA-MB-453 xenograft tumor model in male SCID mice[1]
Dosage: 25, 50 mg/kg
Administration: IP; daily; for 75 days
Result: Effectively inhibited tumor growth.
Molecular Weight

1095.78

Formula

C61H71ClN8O7S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC(C)([C@H](C1(C)C)NC(C2=CC=C(C=C2)C#CC3CCN(C4CCN(CC4)C(C[C@@H](C5=CC=C(C6=C(C)N=CS6)C=C5)NC([C@H]7N(C[C@@H](C7)O)C([C@@H](C8=CC(C)=NO8)C(C)C)=O)=O)=O)CC3)=O)[C@H]1OC9=CC(Cl)=C(C=C9)C#N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (91.26 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 0.9126 mL 4.5630 mL 9.1259 mL
5 mM 0.1825 mL 0.9126 mL 1.8252 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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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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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: ≥ 2.5 mg/mL (2.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (2.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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).
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

Purity: 99.68%

SDS (251 KB)

COA (247 KB) HNMR (177 KB) RP-HPLC (268 KB)

Handling Instructions (2659 KB)
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. 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 0.9126 mL 4.5630 mL 9.1259 mL 22.8148 mL
5 mM 0.1825 mL 0.9126 mL 1.8252 mL 4.5630 mL
10 mM 0.0913 mL 0.4563 mL 0.9126 mL 2.2815 mL
15 mM 0.0608 mL 0.3042 mL 0.6084 mL 1.5210 mL
20 mM 0.0456 mL 0.2281 mL 0.4563 mL 1.1407 mL
25 mM 0.0365 mL 0.1825 mL 0.3650 mL 0.9126 mL
30 mM 0.0304 mL 0.1521 mL 0.3042 mL 0.7605 mL
40 mM 0.0228 mL 0.1141 mL 0.2281 mL 0.5704 mL
50 mM 0.0183 mL 0.0913 mL 0.1825 mL 0.4563 mL
60 mM 0.0152 mL 0.0760 mL 0.1521 mL 0.3802 mL
80 mM 0.0114 mL 0.0570 mL 0.1141 mL 0.2852 mL
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ARD-61 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-612316837-08-6ARD61ARD 61PROTACsAndrogen ReceptorProgesterone ReceptorApoptosisNR3C3MDA-MB-453cullinE3ligaseHCC1428MCF-7BT-549MDA-MB-415Inhibitorinhibitorinhibit

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