| Identification | Back Directory | [Name]
FGTI-2734 | [CAS]
1247018-19-4 | [Synonyms]
FGTI-2734
2-Pyridinesulfonamide, N-[2-[(4-cyano-2-fluorophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl]-N-(cyclohexylmethyl)- | [Molecular Formula]
C26H31FN6O2S | [MDL Number]
MFCD32174296 | [MOL File]
1247018-19-4.mol | [Molecular Weight]
510.63 |
| Chemical Properties | Back Directory | [Boiling point ]
770.1±70.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);97.92(Max Conc. mM) | [form ]
Solid | [pka]
6.60±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor. It can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors. | [Uses]
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1]. | [in vivo]
FGTI-2734 (intraperitoneally; 100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors[1]. | Animal Model: | Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1] | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneally; daily; for 18 to 25 days | | Result: | Inhibited tumor growth in mutant KRAS-dependent tumors. |
| [target]
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. | [References]
[1] Kazi A, et al. Dual farnesyl and geranylgeranyl transferase inhibitor thwarts mutant KRAS-driven patient-derived pancreatic tumors. Clin Cancer Res. 2019 Jun 21. DOI:10.1158/1078-0432.CCR-18-3399 |
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