JJ-450

JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant ARF876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as ARF876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100).

2020353-42-6

12352005

Androgen Receptor

Vitamin D Related/Nuclear Receptor

Cancer

O=C(N1CCN(C2=C(C=CC(Cl)=C2)C)CC1)[C@H]3[C@@H](C4=CC=C(C=C4)F)C3

C21H22ClFN2O

372.86

[1]Wu Z, et al. A novel androgen receptor antagonist JJ-450 inhibits enzalutamide-resistant mutant ARF876L nuclear import and function. Prostate. 2020 Mar;80 (4) :319-328.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-403733C/

Reference compound1

No Development Reported