A-176120 is a selective inhibitor of farnesyl transferase ( IC 50 =1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI ( IC 50 =423 nM), GGTaseII ( IC 50 =3000 nM), and SSase ( IC 50 >10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells ( ED 50 =1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion.
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