产品介绍
Product Description
Biochem/physiol Actions
AG14361 is a potent oly(ADP-ribose) polymerase-1 inhibitor (human PARP-1 Ki = 5.8 nM) that suppresses 25 μM MNNG-induced PARP-1 activity (NAD+ depletion = 70% without vs.12% with 0.4 μM AG14361; 87% reduced ADP-ribose polymer induction with 0.4 μM AG14361) and greatly amplifies temozolomide and topotecan cytotoxicity (2.2- and 2.0-fold lower IG50, respectively, with 0.4 μM AG14361) in A549 cultures. AG14361 is shown to selectively kill BRCA2-deficient cells over BRCA2-expressing cells both in cultures (1-10 μM) and in mice in vivo (25 mg/10 mL/kg/d ip).
Potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor in vitro and in vivo.
技术参数
Specifications
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (warmed) |
| storage temp. | 2-8°C |
| SMILES string | O=C1C2=C3C(N=C(N3CCN1)C4=CC=C(C=C4)CN(C)C)=CC=C2 |
| InChI | 1S/C19H20N4O/c1-22(2)12-13-6-8-14(9-7-13)18-21-16-5-3-4-15-17(16)23(18)11-10-20-19(15)24/h3-9H,10-12H2,1-2H3,(H,20,24) |
| InChI key | SEKJSSBJKFLZIT-UHFFFAOYSA-N |
