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Tipifarnib (R115777, Zarnestra)


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CAS Number: 192185-72-1

Molecular Formula: C27H22Cl2N4O

Molecular Weight: 489.4

Chemical Name: 1-[[(6R,7R)-7-[[(2Z)-(5-Amino-1,2,4-thiadiazol-3-yl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-imidazo[1,2-b]pyridazinium hydroxide inner salt.

Tipifarnib (Zarnestra) is a farnesyltransferase inhibitor with an IC50 of 0.6 nM. It is a nonpeptidomimetic quinolinone with potential antineoplastic activity. It binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, it prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.

Tipifarnib (R115777), an inhibitor of human protein farnesyltransferase (PFT), is shown to be a highly potent inhibitor of Trypanosoma cruzi growth (ED50 = 4 nM)


1. O.Hucke, et al: J. Med. Chem., 2005, 48 (17), pp 5415–5418 "The Protein Farnesyltransferase Inhibitor Tipifarnib as a New Lead for the Development of Drugs against Chagas Disease" 

2. Martin LA et al.: Mol Cancer Ther. 2007 Sep;6(9):2458-67. "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."

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