FHD-286

FHD-286 is an inhibitor of Brahma homolog (BRM), also known as SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), and Brahma-related gene 1 (BRG1), also known as SMARCA4. It induces differentiation of, and reduces viability in, MV4-11 and MOLM-13 acute myeloid leukemia (AML) cells, which express mixed-lineage leukemia 1 (MLL1) rearrangements, and OCI-AML-3 AML cells, which express mutant nucleophosmin 1 (NPM1), when used at a concentration of 30 nM. FHD-286 (100 nM) decreases BRG1-chromatin and BRM-chromatin associations in MOLM-13 cells. In vivo, FHD-286 (1.5 mg/kg) decreases tumor burden and increases survival in patient-derived xenograft (PDX) mouse models of AML when used alone or in combination with venetoclax (ABT-199, Cay-16233), OTX015 (Cay-15947), SNDX-5613 (Cay-40758), or decitabine (Cay-11166).Formal Name: N-[(1S)-2-[[4-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-2-pyridinyl]-2-thiazolyl]amino]-1-(methoxymethyl)-2-oxoethyl]-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide. CAS Number: 2671128-05-3. Molecular Formula: C24H30N6O6S2. Formula Weight: 562.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Slightly soluble: 0.1-1 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml. SMILES: O=C(NC1=NC(C2=CC=CC(N3C[C@@H](C)O[C@@H](C)C3)=N2)=CS1)[C@@H](NC(C4=CN(S(C)(=O)=O)C=C4)=O)COC. InChi Code: InChI=1S/C24H30N6O6S2/c1-15-10-29(11-16(2)36-15)21-7-5-6-18(25-21)20-14-37-24(27-20)28-23(32)19(13-35-3)26-22(31)17-8-9-30(12-17)38(4,33)34/h5-9,12,14-16,19H,10-11,13H2,1-4H3,(H,26,31)(H,27,28,32)/t15-,16+,19-/m0/s1. InChi Key: JBLQNFBXKOAIHG-FCEWJHQRSA-N.