ARV-110 | Androgen receptor degrader

ARV-110 chemical structure

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ARV-110 (2222112-77-6) is a CRBN-based PROTAC protein degrader that recruits the cereblon-containing E3 ubiquitin ligase to direct the proteasomal degradation of the androgen receptor (AR). It selectively degrades wild-type AR and most clinically relevant mutants with low nM potency.1 ARV-110 is the first PROTAC to enter the clinic.2  Analytical methods suitable for pharmacokinetic studies have been developed.3 Caution: May be teratogenic. Pregnant women should avoid all contact with this substance.

References/Citations:

  1. Snyder et al. (2024), Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting Chimera Androgen Receptor Degrader; Mol. Cancer Ther., 24 511
  2. Jia and Han (2023), Targeting androgen receptor degradation with PROTACs from bench to bedside; Biomed. Pharmacother., 158 114112
  3. Nguyen et al. (2022), Development of an LC-MS/MS Method for ARV-110, a PROTAC Molecule, and Applications to Pharmacokinetic Studies; Molecules, 27 1977

 

2222112-77-6, androgen receptor degrader, androgen receptor protac, ARV-110, ARV-110 supplier, ARV110, Bavdegalutamide, Bavdegalutamide supplier
Alternate Name:
Bavdegalutamide

Safety Data Sheet:

N/A

Product Data Sheet:

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ARV-110 (2222112-77-6) is a CRBN-based PROTAC protein degrader that recruits the cereblon-containing E3 ubiquitin ligase to direct the proteasomal degradation of the androgen receptor (AR). It selectively degrades wild-type AR and most clinically relevant mutants with low nM potency.1 ARV-110 is the first PROTAC to enter the clinic.2  Analytical methods suitable for pharmacokinetic studies have been developed.3 Caution: May be teratogenic. Pregnant women should avoid all contact with this substance.

References/Citations:

  1. Snyder et al. (2024), Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting Chimera Androgen Receptor Degrader; Mol. Cancer Ther., 24 511
  2. Jia and Han (2023), Targeting androgen receptor degradation with PROTACs from bench to bedside; Biomed. Pharmacother., 158 114112
  3. Nguyen et al. (2022), Development of an LC-MS/MS Method for ARV-110, a PROTAC Molecule, and Applications to Pharmacokinetic Studies; Molecules, 27 1977