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251577-09-0

251577-09-0 structure
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
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

Chemsrc provides CAS#:251577-09-0 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 251577-09-0 | Chemsrc address: https://www.chemsrc.com/en/baike/1491677.html

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