FTI-2153 is the methylester prodrug of FTI-2148, a potent, selective farnesyltransferase (FTase) inhibitor with IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at inhibiting H-Ras (IC50, 10 nM) than Rap1A processing. FTI-2153 is highly effective at suppressing oncogenic H-Ras constitutive activation of mitogen-activated protein kinase and human tumor growth in soft agar. FTI-2153 blocks bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells.
