Formulation: A solid
Formal Name: 1,3-dimethyl-5-[2-(tetrahydro-2H-pyran-4-yl)-1-[2-(trifluoromethoxy)ethyl]-1H-benzimidazol-6-yl]-2(1H)-pyridinone
Purity: ≥98%
Formula Markup: C22H24F3N3O3
Formula Weight: 435,4
Shelf life (days): 1460
CAS Number: 2081072-29-7
Notes: 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.
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