FTI 276 (TFA)

FTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC₅₀ of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma^[1][2]. IC50 & Target:IC50: 0.9 nM (PFT, Plasmodium falciparum), 0.5 nM (PFT, human)^[1]. In Vitro:FTI 276 TFA potently and selectively inhibits FTase in vitro, with 100-fold greater activity against FTase than GGTase I^[1].
FTI 276 TFA inhibits farnesylation of K-Ras4B in vitro with 10-fold lower potency than it inhibits farnesylation of H-Ras^[1].
FTI 276 TFA potently inhibits Daudi cell-derived FTase with an IC₅₀ of 500 pM and shows 100-fold selectivity over Daudi cell-derived GGTase I, which it inhibits with an IC₅₀ of 50 nM^[2]. In Vivo:FTI 276 TFA (50 mg/kg/day; subcutaneous; constant rate; 30 days) produces significant chemotherapeutic efficacy in established NNK-induced lung adenomas in male A/J mice^[1].