| Name | FTI-277 hydrochloride |
| 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. |
| 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) |
| 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. |
| 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. |
| Storage | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 12 mg/mL (24.79 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.82 mM), Sonication is recommended.
H2O : 14 mg/mL (28.92 mM), Sonication is recommended.
DMSO : 145 mg/mL (299.54 mM), Sonication is recommended.
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| Keywords | Ras | Inhibitor | inhibit | GGTase I | FTI-277 Hydrochloride | FTI277 Hydrochloride | FTI-277 | FTI277 | FTI 277 Hydrochloride | FTI 277 | Ftase | Farnesyl Transferase | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | D(+)-Raffinose pentahydrate | Metronidazole | Formamide | Dimethyl phthalate | Daraxonrasib | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Viral Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
