VE-821

Description: VE-821 is a novel potent and highly selective ATP competitive protein kinase inhibitor of ATR (ataxia telangiectasia mutated and Rad3 related) with Ki and IC50 of 13 nM and 26 nM in cell-free assays, it shows inhibition of H2AX phosphorylation, and had minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kgamma. VE-821 inhibited radiation- and gemcitabine-induced phosphorylation of Chk1, confirming inhibition of ATR signaling. Consistently, VE-821 significantly enhanced the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and gemcitabine under both normoxic and hypoxic conditions.

References: Nat Chem Biol. 2011 Apr 13; 7(7):428-30; J Med Chem. 2011 Apr 14; 54(7):2320-30.

VE-821; VE 821; VE821;

Chemical Name: 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide

SMILES Code: O=C(C1=NC(C2=CC=C(S(=O)(C)=O)C=C2)=CN=C1N)NC3=CC=CC=C3