ARD-2051

ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) [1].

Product Specifications

CAS Number

[2632305-17-8]

UNSPSC

12352005

Target

Androgen Receptor; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ard-2051.html

Purity

98.57

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(C1=C2C=CC(N3CC(N4CCN(C(C5=CC=C(C=C5)N6CCC7(CC6)CN([C@H](C7)C)C8=CC(Cl)=C(C=C8)C#N)=O)CC4)C3)=C1)N(C2=O)C9C(NC(CC9)=O)=O

Molecular Formula

C43H45ClN8O5

Molecular Weight

789.32

References & Citations

[1]Han X, et al. Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2023 Jul 13;66 (13) :8822-8843.