FTI-2148 diTFA CAS#: 817586-01-9

Usage And Synthesis

Uses

FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively[1].

in vivo

FTI-2148 (intraperitoneal injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model^[1]. FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model^[1]. FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model^[3]. FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85-88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings^[3].

Animal Model:	Rastransgenic mouse model^[3]
Dosage:	100 mg/kg/day
Administration:	Subcutaneousinjection; 100 mg/kg/day; 14 days
Result:	Reduced regression by 87 ± 3% of mammary carcinomas in mice.

References

[1] Sun J, et al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine.Cancer Res.1999 Oct 1;59(19):4919-26. PMID:10519405
[2] Carrico D, et al.In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability.Bioorg Med Chem.2004 Dec 15;12(24):6517-26. DOI:10.1016/j.bmc.2004.09.020
[3] 3.Sun J, et al. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.Cancer Res. 2003 Dec 15;63(24):8922-9. PMID:14695209

FTI-2148 diTFA

Usage And Synthesis

FTI-2148 diTFA Supplier

Related Product Information