JNJ-63576253 (TRC-253)

JNJ-63576253 can inhibit transcriptional activity in reporter assays, cellular proliferation, and AR downstream target gene expression, as a potent and selective next-generation AR pathway inhibitor. ^{<a class="sref" href="#s_ref">[1]</a>}

LNCaP AR/cs, LNCaP F877L, VCaP, and PC3 are seeded at densities of 5,000 or 250 cells per well into 96-well plates and incubated overnight. Following compound treatment, the cells are incubated for 6 days for assessing proliferation. For transcriptional reporter assays, LNCaP reporter lines are seeded at a density of 10,000 cells per well, incubated overnight, then treated for 24 hours with JNJ-63576253 in the presence of 0.1 nmol/L R1881. After treatment, cells are assayed using the SteadyGlo-luciferase Kit.

JNJ-63576253 causes tumor growth inhibition in an enzalutamide-resistant LNCaP F877 L xenograft model. ^{<a class="sref" href="#s_ref">[1]</a>}