JJ-450 [CAS 2020353-42-6]

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]

C21H22ClFN2O

372.86

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

Androgen Receptor

Room temperature