FTI 277 HCl
Molecular Weight(MW): 484.07
FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.
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(A) HCT 116 cells were treated with Tram (0, 30, or 60 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD. (B) SW480 and MDA-MB-231 cells were treated with Tram (0, 80, 160 nM), and then treated with 10 μM FTI-277/4 μM GGTI-298 or vehicle control for 48 hr. CCK8 assays were performed to assess cell proliferation and growth. The data from a representative example of three independent experiments are presented as the mean±SD.
Cancer Lett, 2018, 442:202-212. FTI 277 HCl purchased from Selleck.
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|Description||FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.|
FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and blocks constitutive MAPK activation in H-RasF cells.  FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells.  FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells.  In SH-SY5Y cells, FTI-277 diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation. 
|In vivo||In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia. |
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.
-  Lerner EC, et al. J Biol Chem. 1995, 270(45), 26802-26806.
-  Bernhard EJ, et al. Cancer Res. 1996, 56(8), 1727-1730.
-  Bolick SC, et al. Leukemia. 2003, 17(2), 451-457
|In vitro||DMSO||96 mg/mL (198.31 mM)|
|Water||17 mg/mL (35.11 mM)|
|Ethanol||14 mg/mL warmed (28.92 mM)|
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