A-800141 is a potent, highly specific, orally bioavailable MetAP2 inhibitor with IC50 of 12 nM, shows no inhibition for MetAP1 (IC50>30 uM); also shows a greater selectivity against other aminopeptidases, as well as a CEREP panel of >80 receptors; causes the formation of GAPDH variants with an unprocessed N-terminal methionine in cell cultures in vitro, exhibits an antiangiogenesis effect and a broad anticancer activity in a variety of tumor xenografts including B cell lymphoma, neuroblastoma, and prostate and colon carcinomas, either as a single agent or in combination with cytotoxic agents; blocks tumor growth and MetAP2 activity in mouse models, which are causally connected to MetAP2 inhibition in vivo.
