251577-09-0

251577-09-0 structure

Name: FTI-2148
Chemical Name: N-[(5-{[(1H-Imidazol-4-ylmethyl)amino]methyl}-2'-methyl-2-biphenylyl)carbonyl]-L-methionine
CAS Number: 251577-09-0
Molecular Formula: C₂₄H₂₈N₄O₃S
Molecular Weight: 452.569
Catalog: Signaling Pathways Metabolic Enzyme/Protease Farnesyl Transferase
Create Date: 2018-06-11 07:55:20
Modify Date: 2024-01-16 16:19:31
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
Synonyms	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

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

251577-09-0	817586-01-9
1217471-51-6	180977-34-8
170006-72-1	1217447-06-7
344900-92-1	170006-73-2
928658-23-5	13700-81-7