FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).

GGT1:1.7 μM, FT-1:1.4 nM

FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all three RAS-transformed NIH3T3 cells [1]. FTI-2148 is effective against P. falciparum PFT (protein farnesyltransferase), Mammalian PFT (protein farnesyltransferase), and Mammalian PGGT-I (geranylgeranyltransferase-I) with IC50s of 15 nM, 0.82 nM, and 1700 nM, respectively [2].

FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model. FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 14 days) causes breast tumor regression in a?ras?transgenic mouse model. FTI-2148 (intraperitoneal?injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model [1]. FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 4 days) causes 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo?settings [3].