A-800141 is an orally active and selective MetAP2 inhibitor with an IC 50 of 12 nM. A-800141 has weak inhibitory activity for MetAP1 ( IC 50 : 36 μM). GAPDH can be used as a biomarker to monitor the MetAP2 inhibition of A-800141. A-800141 has antiangiogenic and anticancer activity in a variety of xenograft tumor models.