Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 48.00 | |
2 mg | In stock | $ 67.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 185.00 | |
25 mg | In stock | $ 337.00 | |
50 mg | In stock | $ 565.00 | |
100 mg | In stock | $ 793.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 113.00 |
Description | 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. |
Targets&IC50 | FTase:500 pM |
In vitro | In mouse models infected with Hepatitis B Virus (HBV) and Hepatitis D Virus (HDV), FTI-277 administered intraperitoneally at a dosage of 50 mg/kg/day effectively clears Hepatitis D viremia. |
In vivo | In drug-resistant myeloma cells, FTI-277 inhibits cell growth and induces apoptosis. It mitigates the toxicity induced by methamphetamine in SH-SY5Y cells through effects on cell degeneration, activation, the c-Jun N-terminal kinase cascade, and the Ras activation process. FTI-277 inhibits Ras processing (IC50: 100 nM) without affecting the overall cellular prenylation of Rap1A. Additionally, FTI-277 increases post-irradiation apoptosis and enhances the radiation sensitivity of H-ras transformed rat embryo cells. |
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 | 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) |
Synonyms | FTI 277 HCl |
Molecular Weight | 484.07 |
Formula | C22H30ClN3O3S2 |
CAS No. | 180977-34-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 12 mg/mL (24.8 mM)
H2O: 14 mg/mL (28.9 mM)
DMSO: 89 mg/mL (183.9 mM)
You can also refer to dose conversion for different animals. More
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FTI-277 hydrochloride 180977-34-8 Apoptosis GPCR/G Protein MAPK Metabolism Ras Transferase Inhibitor Farnesyl Transferase FTI 277 Ftase FTI-277 Hydrochloride FTI 277 Hydrochloride inhibit FTI277 Hydrochloride FTI-277 FTI277 hydrochloride FTI 277 hydrochloride FTI277 FTI 277 HCl inhibitor