INCB 057643

INCB 057643 is a bromodomain and extra terminal domain (BET) family protein inhibitor. It inhibits binding of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 to an acetylated histone H4 peptide in vitro. INCB 057643 decreases Myc levels in, and inhibits proliferation of, acute myeloid leukemia (AML), diffuse large B cell lymphoma (DLBCL), and multiple myeloma (MM) cells. In vivo, INCB 057643 reduces tumor growth in AML, DLBCL, and MM mouse xenograft models. It also reduces tumor growth when administered alone or in combination with docetaxel (Cay-11637) or enzalutamide (MDV 3100, Cay-11596) in a 22Rv1 castration-resistant prostate cancer (CRPC) mouse xenograft model.Formal Name: 8-(6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-2,2,4-trimethyl-6-(methylsulfonyl)-2H-1,4-benzoxazin-3(4H)-one. CAS Number: 1820889-23-3. Molecular Formula: C20H21N3O5S. Formula Weight: 415.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 226, 257 nm. SMILES: O=C1C2=C(C(C3=C(OC(C)(C)C(N4C)=O)C4=CC(S(C)(=O)=O)=C3)=CN1C)C=CN2. InChi Code: InChI=1S/C20H21N3O5S/c1-20(2)19(25)23(4)15-9-11(29(5,26)27)8-13(17(15)28-20)14-10-22(3)18(24)16-12(14)6-7-21-16/h6-10,21H,1-5H3. InChi Key: VZSAMEOETVNDQH-UHFFFAOYSA-N.