FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

FTase:500 pM

在感染乙型肝炎病毒和丁型肝炎病毒的小鼠体内,FTI-277（50 mg/kg/day,i.p.）可有效清除丁型肝炎病毒血症.

在耐药骨髓瘤细胞中,FTI-277对细胞生长有抑制作用,还诱导细胞凋亡。在SH-SY5细胞中,FTI-277对细胞退化、活化、c-Jun-N端激酶级联和Ras激活过程中甲基苯丙胺诱导的毒性有减弱作用。FTI-277抑制Ras加工（IC50：100 nM）,但对全细胞中四异戊二烯化Rap1A加工无影响。FTI-277导致辐射后细胞凋亡增加,并使H-ras转化的大鼠胚胎细胞的辐射敏感性增加。

FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.

Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. (Only for Reference)