A PROTAC that drives androgen receptor degradation
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ARV-766

Item No. 41985

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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-fluoro-benzamide
CAS Number
2750830-09-0
Synonyms
  • Luxdegalutamide
Molecular Formula
C45H54FN7O6
Formula Weight
808.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
CC(C)([C@H](C1(C)C)NC(C2=CC=C(N3CCC(CC3)CN4CCN(C5=CC=C(C(F)=C5)C(N[C@H]6CCC(NC6=O)=O)=O)CC4)C=C2)=O)[C@H]1OC7=CC(OC)=C(C=C7)C#N
InChi Code
InChI=1S/C45H54FN7O6/c1-44(2)42(45(3,4)43(44)59-33-12-8-30(26-47)37(25-33)58-5)50-39(55)29-6-9-31(10-7-29)52-18-16-28(17-19-52)27-51-20-22-53(23-21-51)32-11-13-34(35(46)24-32)40(56)48-36-14-15-38(54)49-41(36)57/h6-13,24-25,28,36,42-43H,14-23,27H2,1-5H3,(H,48,56)(H,50,55)(H,49,54,57)/t36-,42-,43-/m0/s1
InChi Key
RDPPBRKNBBXPNZ-FMPIRMQTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ARV-766 is a proteolysis-targeting chimera (PROTAC) that drives androgen receptor degradation.1 It induces degradation of the androgen receptor in VCaP cells with a half-maximal degradation concentration (DC50) value of less than 1 nM. ARV-766 inhibits tumor growth in various LNCaP and VCaP prostate cancer mouse xenograft models, including an enzalutamide-insensitive, non-castrated VCaP model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Snyder, L., Lee, S.H., Neklesa, T.K., et al. Discovery of ARV-766, an androgen receptor degrading PROTAC® for the treatment of men with metastatic castration resistant prostate cancer. Proceedings of the American Association for Cancer Research Annual Meeting Part 1 (Regular and Invited Abstracts (2023).