After further optimization, they finally obtained compound A485 with nanomolar affinity, high selectivity, drug-like properties, and oral bioavailability.344 The compound has been demonstrated to have significant inhibitory activity in NSCLC, mantle cell lymphoma, multiple myeloma, non-Hodgkin’s lymphoma cells, and AR-positive prostate cancer cells.345–347 Similar with C646, A485 can enhance the tumor-killing effect of PD-L1 antibody.348 Mechanistically, it blocks the acetylation of histone H3 at the PD-L1 promoter and inhibits its transcription. Here, AR is linked to prostate cancer.