ARV-766 98% Purity PROTAC Protein Degrader Androgen Receptor Degrader CAS 2750830-09-0 CRPC Research

Product Overview

ARV-766 (Luxdegalutamide) is a novel, orally bioavailable proteolysis targeting chimera (PROTAC) designed to selectively degrade the androgen receptor (AR). It represents a second-generation AR-targeting PROTAC developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Unlike traditional AR antagonists that simply inhibit receptor function, ARV-766 recruits the E3 ubiquitin ligase complex to the AR protein, triggering its ubiquitination and subsequent proteasomal degradation.

Chemically, ARV-766 has the molecular formula C₄₅H₅₄FN₇O₆ and a molecular weight of 807.95 g/mol. It is a white to off-white solid with good solubility in DMSO and organic solvents. The compound structure consists of three key components: an AR-binding ligand, an E3 ligase-binding moiety, and a linker connecting the two.

Mechanism of Action

ARV-766 exerts its therapeutic effects through the PROTAC mechanism:

• Bifunctional Molecule: Simultaneously binds to both the androgen receptor and an E3 ubiquitin ligase

• Ternary Complex Formation: Brings AR and E3 ligase into close proximity, forming a ternary complex

• Ubiquitination: The E3 ligase catalyzes ubiquitination of the AR protein

• Proteasomal Degradation: Ubiquitinated AR is recognized and degraded by the proteasome

• Broad Mutant Activity: Degrades both wild-type AR and clinically relevant AR mutants including L702H, T878A, and H875Y, which are associated with resistance to current anti-androgen therapies

This degradation-based approach offers potential advantages over traditional AR antagonists, including more complete pathway inhibition and activity against resistance mutations.

Research Applications & Clinical Development

ARV-766 represents a significant advance in targeted protein degradation therapy:

• Prostate Cancer Research: Valuable tool for studying AR signaling and treatment resistance in CRPC

• PROTAC Technology Development: Serves as a benchmark compound for PROTAC optimization and development

• Resistance Mechanism Studies: Useful for investigating mechanisms of anti-androgen resistance

• Combination Therapy Research: Supports studies of PROTACs in combination with other cancer therapies

ARV-766 has shown promising results in clinical trials, demonstrating significant PSA reductions and anti-tumor activity in mCRPC patients. The development of AR-targeting PROTACs represents a new paradigm in prostate cancer treatment, with the potential to overcome resistance to current standard-of-care therapies.

Quality Specifications

Our ARV-766 is manufactured under strict quality control conditions:

• Purity: ≥98.0% determined by HPLC

• Identity confirmed by ¹H NMR and high-resolution mass spectrometry

• Water content: ≤0.5%

• Residual solvents: Meet ICH Q3C guidelines

• Enantiomeric purity: ≥99%

• Each batch accompanied by comprehensive Certificate of Analysis (COA)

• Stable for 24 months when stored at 4°C in sealed containers protected from light and moisture

Packaging & Shipping

We offer flexible packaging options to meet diverse customer needs:

• Research quantities: 10mg, 50mg, 100mg amber glass vials

• Bulk quantities: 1g, 5g amber glass bottles

• Custom packaging available upon request

• Shipped with appropriate temperature control

• International shipping available with proper documentation

• Cold chain shipping available for temperature-sensitive orders