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Tipifarnib

Cat. No. M1885
Tipifarnib Structure
Synonym:

IND 58359; R115777

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 110  USD110 In stock
2mg USD 55  USD55 In stock
5mg USD 100  USD100 In stock
10mg USD 180  USD180 In stock
100mg USD 880  USD880 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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.
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Harousseau JL, et al. Blood. A randomized phase 3 study of tipifarnib compared with best supportive care, including hydroxyurea, in the treatment of newly diagnosed acute myeloid leukemia in patients 70 years or older.

[2] Karp JE, et al. Clin Cancer Res. Phase II trial of tipifarnib as maintenance therapy in first complete remission in adults with acute myelogenous leukemia and poor-risk features.

[3] Martin LA, et al. Mol Cancer Ther. The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.

[4] Alsina M, et al. Blood. Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.

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Keywords: Tipifarnib, IND 58359; R115777 supplier, Farnesyl Transferase, inhibitors, activators


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