FTI 277 HCl
For research use only.
CAS No. 180977-34-8
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 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.
Selleck's FTI 277 HCl has been cited by 7 publications
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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 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.|
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|
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