MCI-030 (ADT 061) is a potent, selective PDE10 inhibitor, inhibits recombinant PDE10 using cGMP as a substrate with IC50 of 0.3 uM.
MCI-030 (ADT 061) is specific for PDE10 and shows no appreciably affecting the activity of all other PDE isozymes.
MCI-030 (ADT 061) completely lacked COX-1 or COX-2 inhibitory activity at concentrations up to 50 μM.
MCI-030 (ADT 061) potently inhibited the growth of colon cancer cell lines, HCT116, HT-29, and SW480, with IC50 values of 0.31, 0.33, and 0.37 μM, respectively, but did not appreciably affect the growth of normal colon mucosal (NCM460) cells up to 50 μM.
ADT 061 activates cGMP/PKG signaling and suppresses oncogenic β-catenin TCF/LEF transcriptional activity in HT-29 colon cancer cells, blocks Wnt-induced nuclear translocation of β-catenin.
MCI-030 (ADT 061) decreased ovarian cancer cell growth and induced cell cycle arrest and apoptosis in vitro.
MCI-030 (ADT 061) inhibited colon adenomas in the Apc+/Min-FCCC mouse model, orally active.