VE-821 is a potent ATP-competitive inhibitor of ATR with a Ki/IC50 of 13 nM/26 nM. It demonstrates excellent selectivity for ATR with minimal cross-reactivity against related PIKKs such as ATM, DNA-PK, mTOR, and PI3Kγ. This inhibitor also significantly enhances the sensitivity of PSN-1, MiaPaCa-2, and primary PancM pancreatic cancer cells to radiation and Gemcitabine, under both normoxic and hypoxic conditions. ATR inhibition by VE-821 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 for ATR
- Demonstrates 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)