NEO2734

NEO2734 is a dual inhibitor of the bromodomain and extra terminal domain family of proteins (BET) and p300/CREB-binding protein (CBP). 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). 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.Formal Name: 1,3-dimethyl-5-[2-(tetrahydro-2H-pyran-4-yl)-1-[2-(trifluoromethoxy)ethyl]-1H-benzimidazol-6-yl]-2(1H)-pyridinone. CAS Number: 2081072-29-7. Molecular Formula: C22H24F3N3O3. Formula Weight: 435.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly Soluble: 1-10 mg/ml, Ethanol: Sparingly Soluble: 1-10 mg/ml. SMILES: O=C1C(C)=CC(C2=CC3=C(N=C(C4CCOCC4)N3CCOC(F)(F)F)C=C2)=CN1C. InChi Code: InChI=1S/C22H24F3N3O3/c1-14-11-17(13-27(2)21(14)29)16-3-4-18-19(12-16)28(7-10-31-22(23,24)25)20(26-18)15-5-8-30-9-6-15/h3-4,11-13,15H,5-10H2,1-2H3. InChi Key: KPWWFNXRLAAREN-UHFFFAOYSA-N.