Art. -Nr.: HY-139659

ARD-61

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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.

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Reinheit: 99.57%
CAS. Nr.: 2316837-08-6
Formel: C₆₁H₇₁ClN₈O₇S
Molecular Weight:1095.78

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

ARD-61 Chemical Structure

CAS. Nr.: 2316837-08-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	DC₅₀	7.2 nM Compound: 1; ARD-61	Protac activity against VHL/AR in AR-positive human LNCAP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis Protac activity against VHL/AR in AR-positive human LNCAP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis	[PMID: 31804827]
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	DC₅₀	1 nM Compound: 1; ARD-61	Protac activity against VHL/AR in AR-positive human VCaP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis Protac activity against VHL/AR in AR-positive human VCaP cells assessed as induction of AR degradation incubated for 6 hrs by Western blot analysis	[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.

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.

Chemical Information

CAS. Nr. 2316837-08-6
Appearance Solid
Molecular Weight 1095.78
Formel C₆₁H₇₁ClN₈O₇S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9126 mL

4.5630 mL

9.1259 mL

5 mM

0.1825 mL

0.9126 mL

1.8252 mL

10 mM

0.0913 mL

0.4563 mL

0.9126 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lijie Zhao, et al. A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo. Neoplasia. 2020 Oct;22(10):522-532. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

PROTAC Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARD-61 Related Classifications

HY-139659 Related Classifications