AR antagonist 1

SKU: orb1309986

Description

AR antagonist 1 is a potent androgen receptor (AR) antagonist utilized in the development of PROTAC ARD-266. This compound incorporates a VHL E3 ligase ligand, enabling targeted protein degradation. It serves as a key chemical probe for studying AR function in prostate cancer research, both in vitro and in vivo.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1818885-54-9
• MW: 278.777
• Purity: 99.07% (May vary between batches)
• Formula: C₁₅H₁₉ClN₂O
• SMILES: N#CC1=CC=C(O[C@H]2C(C)(C)[C@H](N)C2(C)C)C=C1Cl
• Target: Ligands for E3 Ligase,Ligands for Target Protein for PROTAC,Androgen Receptor
• Solubility: DMSO:60 mg/mL (215.22 mM)

Bioactivity

• Target IC50:
  Androgen receptor:
• In Vitro:
  AR antagonist 1 (compound 29) is the ligand for the target ligase of ARD-266, a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. AR antagonist 1 exhibits micromolar binding affinity to its E3 ligase complex and can be effectively used in designing potent and efficient PROTAC degraders.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E3 ligase-recruiting Moiety, AR antagonist 1, AR antagonist1, AR antagonist-1, Androgen Receptor, androgen receptor, AndrogenReceptor, cancer, Inhibitor, LNCaP, Ligands for E3 Ligase, LigandforE3Ligase, Ligand for E3 Ligase, LigandsforTargetProteinforPROTAC, Ligands for Target Protein for PROTAC, Linker, inhibit, Target Protein-binding Moiety, PROTAC, tumor, VCaP

Compound Identifiers

PubChem CID

118435261