Home Metabolism FTase inhibitor - Transferase inhibitor - Apoptosis related activator - Anti-infection inhibitor FTI 277 HCl For research use only.

FTI 277 HCl

FTI 277 HCl 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 HCl Chemical Structure

FTI 277 HCl Chemical Structure

CAS No. 180977-34-8

Purity & Quality Control

FTI 277 HCl Related Products

Biological Activity

Description FTI 277 HCl 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.
Targets
FTase [1]
(Cell-free assay)
500 pM
In vitro
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models HBV/HDV-transgenic FVB mice
Dosages 50 mg/kg/d
Administration i.p.

Chemical Information & Solubility

Molecular Weight 484.07 Formula

C22H30ClN3O3S2
CAS No. 180977-34-8 SDF Download FTI 277 HCl SDF
Smiles COC(=O)C(CCSC)NC(=O)C1=C(C=C(C=C1)NCC(CS)N)C2=CC=CC=C2.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (198.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 96 mg/mL

Ethanol : 96 mg/mL


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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.

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