| Identification | Back Directory | [Name]
ARV-766 | [CAS]
2750830-09-0 | [Synonyms]
ARV776
4-[4-[[1-[4-[[[trans-3-(4-Cyano-3-methoxyphenoxy)-2,2,4,4-tetramethylcyclobutyl]amino]carbonyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-N-[(3S)-2,6-dioxo-3-piperidinyl]-2-fluorobenzamide | [Molecular Formula]
C45H54FN7O6 | [MOL File]
2750830-09-0.mol | [Molecular Weight]
807.95 |
| Chemical Properties | Back Directory | [Boiling point ]
993.4±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml | [form ]
Solid | [pka]
10.58±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer[1][2]. | [in vivo]
Luxdegalutamide exhibits anti-tumor activity in mouse LNCaP and VCaP xenograft models[2]. | [References]
[1] Snyder L, et al. In vitro evaluation of PROTAC? degrader ARV-766 for cytochrome P450-and transporter-mediated drug-drug interaction[J]. Drug Metabolism and Pharmacokinetics, 2024, 55: 100881.
[2] Snyder L, et al. Abstract ND03: Discovery of ARV-766, an androgen receptor degrading PROTAC? for the treatment of men with metastatic castration resistant prostate cancer[J]. Cancer Research, 2023, 83(7_Supplement): ND03-ND03. |
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