A-176120

Description

A-176120 is a selective inhibitor of farnesyl transferase IC50=1.2 nM based on a farnesyl pyrophosphate FPP analog, with superior selectivity against GGTaseI IC50=423 nM , GGTaseII IC50=3000 nM , and SSase IC50 10 ?M. A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells ED50=1.6 and 0.5 ?M, respectively . A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion.