VE-821 is a potent ATP-competitive inhibitor of ATR, with Ki/IC50 values of 13 nM/26 nM. It demonstrates excellent selectivity for ATR, showing minimal cross-reactivity against related PIKKs such as ATM, DNA-PK, mTOR, and PI3Kγ.
- Shows minimal cross-reactivity against related PIKKs ATM, DNA-PK, mTOR, and PI3Kγ
- Significantly enhances the sensitivity of PSN-1, MiaPaCa-2, and primary PancM pancreatic cancer cells to radiation and Gemcitabine
- ATR inhibition by VE-821 leads to inhibition of radiation-induced G2/M arrest in cancer cells
- Inhibits phosphorylation of Chk1 (Ser 345) in PSN-1 and MiaPaCa-2 cells after treatment with Gemcitabine, radiation, or both