FTI 277 HCl

Catalog No.S7465

FTI 277 HCl Chemical Structure

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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Cited by 3 Publications

1 Customer Review

  • (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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Biological Activity

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.
Targets
FTase [1]
(Cell-free assay)
500 pM
In vitro

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. [1] FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. [2] FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. [3] 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. [4]

In vivo In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia. [5]

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[3]

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  • Cell lines: 8226, U266, and H929 multiple myeloma cell lines
  • Concentrations: ~10 μM
  • Incubation Time: 96 hours
  • Method:

    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)
Animal Research:

[5]

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  • Animal Models: HBV/HDV-transgenic FVB mice
  • Formulation: 5% DMSO, 0.5 mM DTT in sterile saline
  • Dosages: 50 mg/kg/d
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (198.31 mM)
Water 17 mg/mL (35.11 mM)
Ethanol 14 mg/mL warmed (28.92 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 484.07
Formula

C22H30ClN3O3S2

CAS No. 180977-34-8
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID