AZD7762

AZD7762 is a potent and selective inhibitor of checkpoint kinases 1 and 2 (IC50 = 5 nM for both) .1 It abrogates DNA damage-induced S and G2 checkpoints and enhances the efficacy of DNA damaging agents such as gemcitabine and irinotecan. AZD7762 also enhanced the radiation sensitivity of p53-mutant tumor cell lines.2,3 AZD7762 was able to overcome imatinib resistance in CML cells.4 AZD7762 has also been reported to be a potent inhibitor of MEKK2 (MAP3K2) – IC50 = 20 nM.5 It has also recently been shown to inhibit antigen-stimulated degranulation from RBL-2H3 (IC50 = 28 nM) and BMMCs (IC50 = 99 nM) as well as suppressing degranulation of LAD2 human mast cells (IC50 = 50 nM) via Syk suppression through inactivation of Lyn and Fyn kinases.6