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Description: FTI 277 HCl (FTI-277; FTI277), the HCl salt of FTI 277, is a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B which is a novel, potent and selective farnesyltransferase (FTase) inhibitor with antiviral activity. It inhibits FTase with an IC50 of 500 pM. It shows > 100-fold selectivity for FTase over the closely related GGTase I. FTI-277 is a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.FTI-277 inhibits the processing of both oncogenic and normal Ras. FTI-277 was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells.
References: J Biol Chem. 1995 Nov 10; 270(45):26802-6; Cancer Res. 1996 Apr 15; 56(8):1727-30; J Clin Invest. 2003 Aug; 112(3):407-14.
Related CAS: 1217447-06-7 (TFA); 170006-73-2 (free base);
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