Art. -Nr.: HY-133020

ARD-266

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ARD-266 is a highly potent and von Hippel-Lindau 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. ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(Pink: Target protein ligand; Blue: VHL E3 ligase ligand; Black: linker).

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Reinheit: 99.94%
CAS. Nr.: 2666951-70-6
Formel: C₅₂H₅₉ClN₆O₇
Molecular Weight:915.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ARD-266 Chemical Structure

CAS. Nr.: 2666951-70-6

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

Biologische Aktivität

Beschreibung

ARD-266 is a highly potent and von Hippel-Lindau 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]. ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. (Pink: Target protein ligand; Blue: VHL E3 ligase ligand; Black: linker).

IC₅₀ & Target^[1]

VHL

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	DC₅₀	0.5352 nM Compound: 11; ARD-266	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: 11; ARD-266	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	0.9686 nM Compound: 11; ARD-266	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	6 nM Compound: 11; ARD-266	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-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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 2666951-70-6
Appearance Solid
Molecular Weight 915.51
Formel C₅₂H₅₉ClN₆O₇
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (109.23 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

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. 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 5 mg/mL (5.46 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (5.46 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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 (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0923 mL	5.4614 mL	10.9229 mL	27.3072 mL
	5 mM	0.2185 mL	1.0923 mL	2.1846 mL	5.4614 mL
	10 mM	0.1092 mL	0.5461 mL	1.0923 mL	2.7307 mL
	15 mM	0.0728 mL	0.3641 mL	0.7282 mL	1.8205 mL
	20 mM	0.0546 mL	0.2731 mL	0.5461 mL	1.3654 mL
	25 mM	0.0437 mL	0.2185 mL	0.4369 mL	1.0923 mL
	30 mM	0.0364 mL	0.1820 mL	0.3641 mL	0.9102 mL
	40 mM	0.0273 mL	0.1365 mL	0.2731 mL	0.6827 mL
	50 mM	0.0218 mL	0.1092 mL	0.2185 mL	0.5461 mL
	60 mM	0.0182 mL	0.0910 mL	0.1820 mL	0.4551 mL
	80 mM	0.0137 mL	0.0683 mL	0.1365 mL	0.3413 mL
	100 mM	0.0109 mL	0.0546 mL	0.1092 mL	0.2731 mL

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ARD-266

PROTAC Library

MCE Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARD-266

PROTAC Library

MCE Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ARD-266 Related Classifications

HY-133020 Related Classifications