Catalog No.: PC-72511Not For Human Use, Lab Use Only.
JNJ-63576253 (TRC-253, JNJ63576253) is a next-generation, potent, selective androgen receptor (AR) antagonist (inhibitor) against wild-type AR (IC50=6.9 nM), AR F877L and other clinically detected ligand binding domain (LBD) point mutations.
JNJ-63576253 (TRC-253, JNJ63576253) is a next-generation, potent, selective androgen receptor (AR) antagonist (inhibitor) against wild-type AR (IC50=6.9 nM), AR F877L and other clinically detected ligand binding domain (LBD) point mutations.
JNJ-63576253 inhibits transcriptional activity in reporter assays, cellular proliferation, and AR downstream target gene expression.
JNJ-63576253 causes tumor growth inhibition (TGI) in an enzalutamide-resistant LNCaP F877 L xenograft model.
JNJ-63576253 displayed an approximately 1,000-fold selectivity versus other nuclear hormone receptors (GR IC50>30 uM).
JNJ-63576253 completely inhibited transiently transfected VP16-AR F877 L with IC50 of 15 nM in HepG2 transcriptional reporter models, JNJ-63576253 completely inhibited AR-mediated transactivation in the presence of 100 pmol/L R1881 (IC50=99 nM).
JNJ-63576253 abrogates cellular proliferation, nuclear translocation, and AR target gene expression in models of human prostate adenocarcinoma.
JNJ-63576253 causes tumor growth inhibition (TGI) in an enzalutamide-resistant LNCaP F877 L xenograft model.
