Synonyms: 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one; AG 14361; AG-14361
Molecular Formula: C19H20N4O
Molecular Weight: 320.39
Linear Structural Formula: C19H20N4O
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: AG14361 is a potent oly(ADP-ribose) polymerase-1 inhibitor (human PARP-1 Ki = 5.8 nM) that suppresses 25 muM MNNG-induced PARP-1 activity (NAD+ depletion = 70% without vs.12% with 0.4 muM AG14361; 87% reduced ADP-ribose polymer induction with 0.4 muM AG14361) and greatly amplifies temozolomide and topotecan cytotoxicity (2.2- and 2.0-fold lower IG50, respectively, with 0.4 muM AG14361) in A549 cultures. AG14361 is shown to selectively kill BRCA2-deficient cells over BRCA2-expressing cells both in cultures (1-10 muM) and in mice in vivo (25 mg/10 mL/kg/d ip).