FTI-2148

FTI-2148 is a RAS C-terminal mimetic dual?farnesyl transferase (FT-1)?and?geranylgeranyl transferase-1 (GGT-1)?inhibitor with?IC₅₀s of 1.4 nM and 1.7 μM, respectively^[1]. IC50 & Target: IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)^[1] In Vitro: FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells^[1].
FTI-2148 is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC₅₀ values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I^[2].
In Vivo: 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; 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^[1].
FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a?ras?transgenic mouse model^[1].
FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 4 days) results in 85-88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo?settings^[3].