| Identification | Back Directory | [Name]
2-Pyridinesulfonamide, N-[2-[(4-cyano-2-fluorophenyl)[(1-methyl-1H-imidazol-5-yl)methyl]amino]ethyl]-N-(cyclohexylmethyl)-, compd. with methanesulfonate (1:1) | [CAS]
2702297-24-1 | [Synonyms]
| [Molecular Formula]
C26H31FN6O2S.CH4O3S | [MOL File]
2702297-24-1.mol | [Molecular Weight]
606.73 |
| Hazard Information | Back Directory | [Uses]
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1]. | [in vivo]
FGTI-2734 mesylate (intraperitoneally; 100 mg/kg/day 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.
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| [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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