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Tipifarnib (Zarnestra)

Catalog No.
Farnesyltransferase inhibitor,potent and specific
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
Evaluation Sample
In stock
In stock
In stock
In stock

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Tipifarnib (also known as Zarnestra or R115777), an orally bioavailable quinolone analog of imidazole heterocyclics, is a potent and specific nonpeptidomimetic competitive inhibitor of farnesyltransferase (FTase), an enezyme mediating post-translational farnesylation of multiple protein substrates involved in tumor cell proliferation. It has demonstrated inhibition of growth and proliferation of a broad range of human tumor models (either wild-type or mutated RAS) via cytostatic rather than cytotoxic activity both in vitro and in vivo. It cell-type dependently induces apoptosis in some neoplastic cell lineages other than acute myeloid leukemia (AML), including multiple myeloma (MM) cell lines and MM cultures from patients.


P.K. Epling-Burnett and Thomas P. Loughran Jr. Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib. Expert Opin Investig Drugs. 2010; 19(5): 689-698

Jean-Pierre Armand, Alan K. Burnett, Johannes Drach, Jean-Luc Harousseau, Bob Lowenberg and Jesus San Miguel. The emerging role of targeted therapy for hematologic malignancies: update on bortezomib and tipifarnib. The Oncologist 2007, 12:281-290

Elzbieta Izbicka, David Campos, Gilbert Carrizales and Amita Patnaik. Biomarkers of anticancer activity of R115777 (tipifarnib, zarnestra) in human breast cancer models in vitro. Anticancer Research 2005; 25: 3215-3224

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.192185-72-1
SynonymsZarnestra,R115777,R-115777,IND 58359
Solubility≥8.16 mg/mL in DMSO, ≥9.16 mg/mL in EtOH with ultrasonic,insoluble in H2O
Chemical Name6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one
SDFDownload SDF
Canonical SMILESCN1C=NC=C1C(C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC(=CC=C5)Cl)C)N
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.


Cell experiment: [1]

Cell lines

Human leukemia cell line THP-1

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

100 ng/ml LPS plus 2 μM tipifarnib. 6 time points (0, 10, 20, 30, 40 and 50h)


Tipifarnib showed significant inhibition of the cytokine/ MMP-9 production as early as 20 h for MCP-1 and IL-6 and 30 h for IL-1β and MMP-9. Tipifarnib showed no significant inhibition of IL-8 production.

Animal experiment : [1]

Animal models

Female BALB/c mice (6–7 weeks old)

Dosage form

Tipifarnib was dissolved in 20% cyclodextran, and 50 mg/kg was orally administered to mice at 24, 17, and 1 h before intraperitoneal injection of 20 μg of LPS per mouse, 1 mg/kg.


After treatment of 2h, tipifarnib significantly inhibited LPS-induced TNF-α production and inhibited 50% of MIP-1α and MCP-1 production. After 3h, tipifarnib inhibited about 50% of IL-6 production and almost complete inhibition of IL-1β production. IL12-p40 and -p70 induction by LPS was also inhibited by tipifarnib at 3 h, whereas IL-10 was not significantly changed at both time points. No effects of tipifarnib on LPS-induced KC were observed, consistent with in vitro results for IL-8.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Xue X, Lai K T A, Huang J F, et al. Anti-inflammatory activity in vitro and in vivo of the protein farnesyltransferase inhibitor tipifarnib. Journal of Pharmacology and Experimental Therapeutics, 2006, 317(1): 53-60.

Biological Activity

Description Tipifarnib (R115777) is a potent and specific inhibitor of farnesyltransferase (FTase) with IC50 of 0.6 nM.
Targets FTase          
IC50 0.6 nM          

Quality Control

Chemical structure

Tipifarnib (Zarnestra)

Related Biological Data

Tipifarnib (Zarnestra)

Related Biological Data

Tipifarnib (Zarnestra)