产品描述:
NEO2734 is a dual inhibitor of the bromodomain and extra terminal domain family of proteins (BET) and p300/CREB-binding protein (CBP).{68792} It binds to bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 (Kds = 3.2, 2.3, and 6.5 nM, respectively), bromodomain testis-specific protein 1 (BRDT1) and BRDT2 (Kds = 3.1 and 25 nM, respectively), and p300 and CBP (Kds = 25 and 23 nM, respectively). NEO2734 inhibits the growth of DU145 prostate cancer cells (IC50 = 1.08 µM) and DU145 cells containing the E3 ubiquitin ligase adapter protein speckle-type POZ protein (SPOP) with a glutamine-to-proline mutation at position 165 (SPOPQ165P; IC50 = 0.69 µM).{68793} It also reduces tumor growth, as well as intratumoral levels of prostate-specific antigen (PSA), in prostate cancer patient-derived xenograft (PDX) mouse models expressing either wild-type SPOP or SPOPQ165P when administered at a dose of 30 mg/kg.