PTC-028

PTC-028 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 OVCAR-4 and OV-90 ovarian cancer cells (IC50s = ~0.1 µM for both). It also induces BMI1 degradation in, and apoptosis of, the same cells in a concentration-dependent manner. PTC-028 reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MDS-L myelodysplastic syndrome cells when used at concentrations of 3 and 0.03 µM, respectively. It reduces tumor growth in a OV-90 orthotopic mouse model of ovarian cancer when administered biweekly at a dose of 15 mg/kg.Formal Name: 6-(5,6-difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]-2-pyrazinamine. CAS Number: 1782970-28-8. Molecular Formula: C19H12F5N5. Formula Weight: 405.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 20 mg/ml, DMSO: 1 mg/ml. lambdamax: 280, 350 nm. SMILES: FC1=C(F)C=C2N(C3=NC(NC4=CC=C(C(F)(F)F)C=C4)=CN=C3)C(C)=NC2=C1. InChi Code: InChI=1S/C19H12F5N5/c1-10-26-15-6-13(20)14(21)7-16(15)29(10)18-9-25-8-17(28-18)27-12-4-2-11(3-5-12)19(22,23)24/h2-9H,1H3,(H,27,28). InChi Key: JEZGPBWIZWPDHP-UHFFFAOYSA-N.