817586-01-9

817586-01-9 structure

817586-01-9 structure

Name: FTI-2148 diTFA
Chemical Name: FTI-2148 diTFA
CAS Number: 817586-01-9
Molecular Formula: C₂₈H₃₀F₆N₄O₇S
Molecular Weight: 680.62
Catalog: Signaling Pathways Metabolic Enzyme/Protease Farnesyl Transferase
Create Date: 2020-06-01 11:09:10
Modify Date: 2024-01-12 21:57:20
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].

Name	FTI-2148 diTFA

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase
Target	IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1]
In Vitro	FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1]. 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[2]. Western Blot Analysis[1] Cell Line: KRAS HRAS, and NRAS-transformed NIH3T3 cells Concentration: 30 μM Incubation Time: Result: Inhibited the prenylation of KRAS and NRAS.
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: Ras transgenic mouse model[3] Dosage: 100 mg/kg/day Administration: Subcutaneous injection; 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. [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]. 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.

Molecular Formula	C₂₈H₃₀F₆N₄O₇S
Molecular Weight	680.62

Hazard Codes	Xi