All AbMole products are for research use only, cannot be used for human consumption.
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
 |
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 |
| Related Farnesyl Transferase Products |
|---|
| LB42708
LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively. |
| Tipifarnib S enantiomer
Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib, Tipifarnib S enantiomer is the less active isomer. |
| L-778123 hydrochloride
L-778123 hydrochloride is a dual inhibitor of FPTase and GGptase-I with IC50 values of 2 nM and 98 nM, respectively. |
| FTI-277 hydrochloride
Fti-277 Hydrochloride, an FTase inhibitor of Farnici transferase, is a highly effective Ras CAAX peptide analog that inhibits H-RAS and K-RAS signal transduction. Fti-277 hydrochloride inhibits hepatitis delta virus (HDV) infection. |
| Manumycin A
Manumycin A is a selective, competitive inhibitor of protein farnesyl transferase (FTase) with respect to farnesylpyrophosphate (Ki=1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A is also an antibiotic. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
