NEO2734 (NEO-2734, EP31670) is a dual inhibitor of pan-BET and CBP/p300 with Kd values of 2-31 nM.
NEO2734 exhibited in vitro antitumor activity in a variety of cancer cell lines derived from different tumor types, especially from prostate cancer, leukemias, and lymphomas.
NEO2734 showed a clear in vitro antitumor activity in DLBCL, which was more potent than either a BET inhibitor (birabresib) or a CBP/EP300 inhibitor (SGC-CBP30).
NEO2734 is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo.
