Bavdegalutamide

Bavdegalutamide
Product Description

 Given these mechanisms of resistance, our goal is to eliminate the AR protein using the PROteolysis TArgeting Chimera (PROTAC) technology. Here we report an orally bioavailable small molecule ARV-110 that leads to ubiquitination and degradation of AR. ARV-110 completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) < 1 nM. PROTAC-mediated AR degradation suppresses the expression of the AR-target genes PSA and FKBP5, inhibits AR-dependent cell proliferation, and induces potent apoptosis in VCaP cells. ARV-110 degrades clinically relevant mutant AR proteins and retains activity in a high androgen environment. In mouse xenograft studies, greater than 90% AR degradation is observed at a 1 mg/kg PO QD dose. Significant inhibition of tumor growth and AR signaling can be achieved in both an intact and castrate setting.

Medsyn (Chengdu) Biotechnology Co., Ltd

  • CN
  • 2023
    On CPHI since
Specifications
  • CAS Registry Number
    2222112-77-6
  • Selling Points
    Experienced Technicians; Product Features
  • Measured In
    gram; kilogram

Medsyn (Chengdu) Biotechnology Co., Ltd

  • CN
  • 2023
    On CPHI since

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