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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 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion[1]. | [References]
[1] Tahir SK, et al. Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue. Eur J Cancer. 2000 Jun;36(9):1161-70. DOI:10.1016/s0959-8049(00)00067-8 |
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