AZD-7648

AZD-7648 is a potent, selective, and orally bioavailable small molecule inhibitor of DNA-dependent protein kinase (DNA-PK). DNA-PK is a critical enzyme involved in the non-homologous end-joining (NHEJ) pathway, which is a primary mechanism for repairing DNA double-strand breaks (DSBs). By inhibiting DNA-PK, AZD-7648 disrupts DNA repair processes, leading to increased DNA damage, apoptosis, and cell cycle arrest in cancer cells. This action sensitizes cancer cells to other DNA-damaging agents, such as doxorubicin and olaparib, and is being investigated for its potential in various advanced cancers. Additionally, AZD-7648 shows promise in enhancing gene targeting efficiency in CRISPR-Cas9 gene editing by shifting DNA repair towards the more precise homology-directed repair (HDR) pathway.

Other names

7-methyl-2-[(7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(oxan-4-yl)purin-8-one7-Methyl-2-((7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino)-9-(tetrahydro‑2H‑pyran‑4‑yl)-7H-purin‑8(9H)-one2230820‑11‑6