MC3343

A DNA methyltransferase inhibitor (IC50s = 9 and 2.8 µM for DNMT1 and the DNMT3A2/DNMT3L complex, respectively), selective for these DNMTs over PRMT1 and G9a-like protein, selectively decreases the viability of U937, Raji, PC3, and MDA-MB-231 cancer cells over isolated PBMCs (IC50s = 4.3, 8.8, 6.6, 9.7, and 57.4 µM, respectively), decreases tumor volume in a PDX mouse model of osteosarcoma at 50 mg/kg when used alone or in combination with doxorubicin. Formulation: A solid. InChI: InChI=1S/C27H23N7O/c1-17-14-25(34-27(28)30-17)32-20-8-5-9-21(16-20)33-26(35)18-6-4-7-19(15-18)31-24-12-13-29-23-11-3-2-10-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34). InChIKey: GRGNBXUBKBUEDX-UHFFFAOYSA-N. SMILES: O=C(C1=CC(NC2=C3C=CC=CC3=NC=C2)=CC=C1)NC4=CC(NC5=NC(N)=NC(C)=C5)=CC=C4