ARD-69

• 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) .

• 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)

• CAS Number:

  [2316837-10-0]