PTC-596

PTC-596 is an inhibitor of B cell-specific Moloney murine leukemia virus integration site 1 (BMI1), which is a member of the polycomb repressive complex 1 (PRC1) that has a role in gene silencing. It inhibits proliferation of MOLM-13 acute myeloid leukemia (AML) and Rec-1 mantle cell lymphoma (MCL) cancer cells (IC50s = 22.4 and 136 nM, respectively). It also induces BMI1 degradation in, and apoptosis of, the same cells. PTC-596 reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MM.1S multiple myeloma cells. It decreases the number of side population cells, a unique cell population with stem-like characteristics, in Rec-1 cells (IC50 = 138 nM). PTC-596 (5 mg/kg, p.o.) increases survival in a MOLM-13 mouse xenograft model.Formal Name: 5-fluoro-2-(6-fluoro-2-methyl-1H-benzimidazol-1-yl)-N4-[4-(trifluoromethyl)phenyl]-4,6-pyrimidinediamine. CAS Number: 1610964-64-1. Synonyms: Unesbulin. Molecular Formula: C19H13F5N6. Formula Weight: 420.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 5 mg/ml. lambdamax: 222, 262, 300 nm. SMILES: FC1=CC2=C(N=C(C)N2C3=NC(NC4=CC=C(C(F)(F)F)C=C4)=C(F)C(N)=N3)C=C1. InChi Code: InChI=1S/C19H13F5N6/c1-9-26-13-7-4-11(20)8-14(13)30(9)18-28-16(25)15(21)17(29-18)27-12-5-2-10(3-6-12)19(22,23)24/h2-8H,1H3,(H3,25,27,28,29). InChi Key: TWLWOOPCEXYVBE-UHFFFAOYSA-N.