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ARD-69

CAT: 0804-HY-114402-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-114402-01Size:1 mg
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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 the treatment 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) .
CAS Number
[2316837-10-0]
Product Name Alternative
Y-39991
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-69.html
Purity
99.61
Solubility
DMSO : ≥ 200 mg/mL
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
Molecular Formula
C62H74ClFN8O7S
Molecular Weight
1129.82
References & Citations
[1]Han X, et al. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 10.|[2]Du W. Advances in AR-targeting chimeras: a case study of proteolysis-targeting chimeras from bench to bedside. Future Med Chem. 2022 Oct;14 (20) :1471-1489.|[3]Xiang, et al. Recent advances in targeting the androgen receptor with PROTACS. 2022 Medicinal Chemistry Reviews (2022) .
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, protect from light, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Von Hippel-Lindau (VHL)

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