Tipifarnib ((IND 58359, R115777) is a potent and selective inhibitor of FTase (farnesyltransferase) with IC50 of 0.86 nM.
Tipifarnib inhibits the farnesylation of lamin B and K-RasB peptide substrates with IC50s of 0.86 nM and 7.9 nM, respectively.
Tipifarnib shows no activity for PGGT1(IC50>50 uM).
Tipifarnib shows sensiticity for tumor cell lines bearing H-ras or N-ras mutations.
Tipifarnib inhibits the growth of tumors bearing mice and orally bioavailable.
