FTI-2148

Modify Date: 2024-01-16 16:19:31

FTI-2148 structure	Common Name	FTI-2148
	CAS Number	251577-09-0	Molecular Weight	452.569
	Density	1.3±0.1 g/cm3	Boiling Point	730.1±60.0 °C at 760 mmHg
	Molecular Formula	C₂₄H₂₈N₄O₃S	Melting Point	N/A
	MSDS	N/A	Flash Point	395.4±32.9 °C

Use of FTI-2148

FTI-2148 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 for FT-1 and GGT-1, respectively[1].

Name	N-[(5-{[(1H-Imidazol-4-ylmethyl)amino]methyl}-2'-methyl-2-biphenylyl)carbonyl]-L-methionine
Synonym	More Synonyms

Description	FTI-2148 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 for FT-1 and GGT-1, 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. Western Blot Analysis[2] 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 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[1]. 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[1]. Animal Model: Ras transgenic mouse model[1] Dosage: 100 mg/kg/day Administration: Subcutaneous injection; 100 mg/kg/day; 14 days Result: Induced regression by 87 ± 3% of mammary carcinomas in mice.
References	[1]. 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. [2]. 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. [3]. Kazi A, et al. Dual Farnesyl and Geranylgeranyl Transferase Inhibitor Thwarts Mutant KRAS-Driven Patient-Derived Pancreatic Tumors.Clin Cancer Res. 2019 Oct 1;25(19):5984-5996.

Density	1.3±0.1 g/cm3
Boiling Point	730.1±60.0 °C at 760 mmHg
Molecular Formula	C₂₄H₂₈N₄O₃S
Molecular Weight	452.569
Flash Point	395.4±32.9 °C
Exact Mass	452.188202
LogP	2.45
Vapour Pressure	0.0±2.5 mmHg at 25°C
Index of Refraction	1.626

Hazard Codes	Xi

L-Methionine, N-[[5-[[(1H-imidazol-4-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-

N-[(5-{[(1H-Imidazol-4-ylmethyl)amino]methyl}-2'-methyl-2-biphenylyl)carbonyl]-L-methionine

N-[(5-{[(1H-imidazol-4-ylmethyl)amino]methyl}-2'-methylbiphenyl-2-yl)carbonyl]-L-methionine

DC Chemicals Limited
China
Product Name: FTI-2148
Price:
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: N-[5-(1H-Imidazol-4-ylmethylaminomethyl)-2\'-methylbiphenyl-2-ylcarbonyl]-L-methionine
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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