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Description: FTI-2148, a RAS C-terminal mimetic, is a novel, potent and highly selective dual inhibitor of farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) with IC50s of 1.4 nM and 1.7 uM, respectively. It has potential antitumor activity. FTI-2148 suppressed the growth of the human lung adenocarcinoma A-549cells in nude mice by 33, 67, and 91% in a dose-dependent manner.Combination therapy of FTI-2148 with either cisplatin, gemcitabine, orTaxol resulted in a greater antitumor efficacy than monotherapy.
References:
1. SunJ, et al. Antitumor efficacy of a novel class of non-thiol-containingpeptidomimetic inhibitors of farnesyltransferase andgeranylgeranyltransferase I: combination therapy with the cytotoxicagents cisplatin, Taxol, and gemcitabine.Cancer Res. 1999 Oct1; 59(19):4919-26.
2. CarricoD, et al.In vitro and in vivo antimalarial activity of peptidomimeticprotein farnesyltransferase inhibitors with improved membranepermeability.Bioorg Med Chem. 2004 Dec 15; 12(24):6517-26.
3. SunJ, et al. Geranylgeranyltransferase I inhibitor GGTI-2154 inducesbreast carcinoma apoptosis and tumor regression in H-Ras transgenicmice.Cancer Res. 2003 Dec 15; 63(24):8922-9.
Related CAS #: 817586-01-9 (TFA) 251577-09-0 (free base)
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