NEO2734, CAS 2081072-29-7

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.

• Artikelnummer: CAY41030-5
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 41030-5
• Verpackungseinheit: 5 mg
• Mengeneinheit: STK