In vitro
As an Tipifarnib (formerly known as R-1 15777), an inhibitor of RAS farnesylation, for the potential treatment of neoplasia. Tipifarnib can inhibit farnesyltransferase with IC50 of 0.6 nM. Tipifarnib is an oral, very potent, and highly selective FTI (farnesyltransferase inhibitors) with a relatively low toxicity pro?le. FTIs function by competitively inhibiting the addition of a farnesyl moiety to several important signaling molecules 3 and thus target multiple pathways, including the RAS pathway implicated in the pathogenesis of solid and hematologic malignancies.
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