AR antagonist 12

AR antagonist 12 (compound 20i) is an orally active androgen receptor antagonist wiith IC50 values of 119.3 μM and 98.2 μM for wt-AR and AR-F877L, respectively. AR antagonist 12 induces a dose-dependent and time-dependent reduction in AR, AR-V7, and PSA protein levels. AR antagonist 1 shows anticancer activuty and can be used for the study of Enzalutamide (HY-70002) -resistant Prostate cancer[1].

Product Specifications

CAS Number

[2902679-42-7]

UNSPSC

12352005

Target

Androgen Receptor

Related Pathways

Vitamin D Related/Nuclear Receptor

Field of Research

Cancer

Smiles

O=C(NC1=CN=C(C(C(F)(F)F)=C1)C#N)[C@@](O)(CN2CC3CCC(N3C4=CC=C(C=C4)C#N)C2)C

Molecular Formula

C24H23F3N6O2

Molecular Weight

484.47

References & Citations

[1]Zhang W, et al. Discovery of Novel Bifunctional Agents as Potent Androgen Receptor Antagonists and Degraders for the Treatment of Enzalutamide-Resistant Prostate Cancer. J Med Chem. 2025 Apr 24;68 (8) :8330-8345.