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Tipifarnib (IND 58359) inhibited Farnesitransferase (FTase) with an IC50 of 0.86 nM. Tipifarnib has potential antitumor activity. Tipifarnib can inhibit exosome release of tumor cells.
2020 Dec.
Zelluläre Seneszenz induziert durch neue zielgerichtete Therapien
Tipifarnib purchased from AbMole
Cancer Cell Int. 2019 Jun 11;19:159.
Harmine suppresses hyper-activated Ras-MAPK pathway by selectively targeting oncogenic mutated Ras/Raf in Caenorhabditis elegans.
Tipifarnib purchased from AbMole
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Source | Universitatsmedizin Berlin (2020 Dec), Figure 4, Tipifarnib (AbMole Bioscience) |
| Method | - | |
| Cell Lines | Vier Zelllinien maligner hamatologischer Erkrankungen (K562, Mec1, RC-K8 und SD-1) | |
| Concentrations | 10-8 M, 10-7 M, 10-6 M, 10-5 M | |
| Incubation Time | 24, 48, 72h | |
| Results | Zusätzlich war nach Behandlung mit ABT-199, Gefitinib, Ibrutinib und Tipifarnib ebenfalls ein Anstieg der CD150-Expression und nach Behandlung mit Ibrutinib und Tipifarnib ein Anstieg der CD133-Expression festzustellen. |
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cells line |
| Preparation method | Cell Growth Assays. Steroid-depleted cells were seeded into 12-well plates at a density of ∼1 × 104 cells per well or into 96-well plates at a density of 4,000 cells per well, in dextran-coated charcoal medium. After 24 h, monolayers were treated with E2 plus inhibitors either alone or in combination. The 12-well plates were treated for 6 days with daily changes. Cell number was then determined using a Z1 Coulter counter (Beckman Coulter). The 96-well plates were treated with a single dose and left for 96 h at which time cell viability was measured using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay as described previously (15). The interaction between R115777 and 4-OH-tamoxifen was analyzed by the median effect plot method described by Chou and Talalay (16). Calculation of the combination index took into account a nonfixed drug ratio and was based on the assumption that the action of the two drugs was mutually nonexclusive for the strict detection of synergism. A combination index < 1 indicates synergism, combination index = 1 indicates additivity, and a combination index > 1 indicates antagonism. Experiments were repeated thrice. |
| Concentrations | 0~1000 nM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | MCF-7 xenografts in Female ovariectomized Ncr foxhead nude mice |
| Formulation | 20% w/v β-cyclodextrin (pH 2.5) |
| Dosages | 50 mg/kg twice daily for 5 consecutive days followed by a 2-day rest period, for a total of 19 days |
| Administration | oral gavage |
| Molecular Weight | 489.39 |
| Formula | C27H22Cl2N4O |
| CAS Number | 192185-72-1 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| FGTI-2734 mesylate
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors. |
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YM-53601 hydrochloride is a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 hydrochloride inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. YM-53601 hydrochloride is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation. |
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