ARV-110 | Androgen receptor degrader

CAS:
 2222112-77-6
Catalog Number:
 10-3016
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
CAS:
2222112-77-6
Catalog Number:
10-3016
Activity:
Androgen receptor degrader
Chemical Names:
N-[trans-4-(3-Chloro-4-cyanophenoxy)cyclohexyl]-6-[4-[[4-[2-(2,6-dioxo-3-piperidinyl)-6-fluoro-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-1-piperazinyl]methyl]-1-piperidinyl]-3-pyridazinecarboxamide
Alternate Name:
Bavdegalutamide
Molecular Weight:
812.30
Molecular Formula:

C41H43ClFN9O6

Solubility:
Soluble in DMSO (25 mg/ml with warming)
Physical Properties:
Pale yellow solid
Purity:

98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 1 year when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

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

 

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