VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 values of 13 nM/26 nM. It exhibits excellent selectivity for ATR, demonstrating minimal cross-reactivity with related PIKKs like ATM, DNA-PK, mTOR, and PI3Kγ. This compound enhances the sensitivity of pancreatic cancer cells (PSN-1, MiaPaCa-2, and primary PancM) to radiation and Gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 also leads to the inhibition of radiation-induced G2/M arrest in cancer cells.
- Potent ATP-competitive inhibitor of ATR (Ki/IC50 of 13 nM/26 nM)
- Exhibits excellent selectivity for ATR with minimal cross-reactivity against related PIKKs
- Enhances sensitivity of pancreatic cancer cells to radiation and Gemcitabine
- Inhibits radiation-induced G2/M arrest in cancer cells
- Inhibits phosphorylation of Chk1 (Ser 345) after specific treatments