MI-463

MI-463 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 15 nM). It inhibits growth of mouse bone marrow cells (BMCs) expressing the MLL fusion protein MLL-AF9 (GI50 = 0.23 µM), as well induces differentiation of MLL-AF9-transformed BMCs. MI-463 (0.75-6 µM) reduces colony formation by patient-derived acute myeloid leukemia (AML) cells. It reduces tumor growth in an MV4-11 mouse xenograft model when administered at a dose of 35 mg/kg.Formal Name: 4-methyl-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-1H-indole-2-carbonitrile. CAS Number: 1628317-18-9. Molecular Formula: C24H23F3N6S. Formula Weight: 484.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Ethanol: soluble. lambdamax: 226, 230, 279, 287 nm. SMILES: N#CC1=CC2=C(C)C(CN3CCC(CC3)NC4=C5C=C(CC(F)(F)F)SC5=NC=N4)=CC=C2N1. InChi Code: InChI=1S/C24H23F3N6S/c1-14-15(2-3-21-19(14)8-17(11-28)31-21)12-33-6-4-16(5-7-33)32-22-20-9-18(10-24(25,26)27)34-23(20)30-13-29-22/h2-3,8-9,13,16,31H,4-7,10,12H2,1H3,(H,29,30,32). InChi Key: DZACSLYTXLZAAF-UHFFFAOYSA-N.