Description
A GCN2 inhibitor (IC50 = 2.4 nM); selective for GCN2 over a panel of 465 kinases but does inhibit MAP2K5, EIF2AK2, and MAP3K20 at 1 µM; in combination with L-aspariginase reduces the viability of MEFs at 1 µM; decreases the levels of ATF4 and phosphorylated GCN2 in combination with L-aspariginase in CCRF CEM leukemia cells at 0.4 µM;, reduces tumor volume in combination with L-aspariginase in CCRF CEM and MV4-11 leukemia mouse xenograft models at 10 mg/kg twice per day