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FGTI-2734

  Cat. No.:  DC32723   Featured
Chemical Structure
1247018-19-4
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Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1247018-19-4
Chemical Name: N-(2-((4-cyano-2-fluorophenyl)((1-methyl-1H-imidazol-5-yl)methyl)amino)ethyl)-N-(cyclohexylmethyl)pyridine-2-sulfonamide
Synonyms: FGTI-2734; FGTI2734; FGTI 2734
SMILES: O=S(C1=NC=CC=C1)(N(CC2CCCCC2)CCN(CC3=CN=CN3C)C4=CC=C(C=C4F)C#N)=O
Formula: C26H31FN6O2S
M.Wt: 510.6324
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: FGTI-2734 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 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1].
Target: IC50: 250 nM (FT) and 520 nM (GGT)[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.
In Vitro: FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells[1]. FGTI-2734 (3-30 μM; 72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells[1]. Apoptosis Analysis[1] Cell Line: MiaPaCa2, L3.6pl and Calu6 cells Concentration: 1, 3, 10, 30 μM Incubation Time: 72 hours Result: Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. Western Blot Analysis[1] Cell Line: KRAS, HRAS, and NRAS-transformed NIH3T3 cells Concentration: 3, 10, 30 μM Incubation Time: 72 hours Result: Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.
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.
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