ART812

ART812 is an inhibitor of DNA polymerase theta (IC50 = 7. nM). It inhibits microhomology-mediated end joining (MMEJ) in a reporter assay using HEK293 cells (EC50 = 240 nM). ART812 (150 mg/kg twice per day) increases blood levels of micronucleated reticulocytes in mice. It inhibits tumor development in a Brca1- and Shld2-knockout MDA-MB-436 breast cancer rat xenograft model of tumor initiation when administered at a dose of 100 mg/kg per day.. Solulibility: DMSO: Soluble: =10 mg/ml: Ethanol: Soluble: =10 mg/ml.