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FTI-2148 diTFA

Catalog No. T11330 CAS 817586-01-9

FTI-2148 diTFA, a dual inhibitor targeting both farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1), functions as a RAS C-terminal mimetic. It exhibits potent inhibitory capabilities with IC50 values of 1.4 nM for FT-1 and 1.7 μM for GGT-1, respectively.

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FTI-2148 diTFA, CAS 817586-01-9

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Biological Description

Chemical Properties

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Description	FTI-2148 diTFA, a dual inhibitor targeting both farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1), functions as a RAS C-terminal mimetic. It exhibits potent inhibitory capabilities with IC50 values of 1.4 nM for FT-1 and 1.7 μM for GGT-1, respectively.
Targets&IC50	GGT-1:1.7 μM , FT-1:1.4 nM
In vitro	FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I.FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells.
In vivo	FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model. 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.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.?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.

Molecular Weight	566.6
Formula	C26H29F3N4O5S
CAS No.	817586-01-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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. 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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

FTI-2148 diTFA 817586-01-9 Others FTI2148 FTI 2148 diTFA FTI2148 diTFA FTI-2148 FTI 2148 inhibitor inhibit

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