Name | FGTI-2734 |
Description | FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors. |
In vitro | 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. FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 50 mg/mL (97.92 mM), Sonication is recommended.
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Keywords | pancreatic | patient-derived | geranylgeranyl | farnesyl | inhibit | Farnesyl Transferase | mimetic | Inhibitor | membrane | Ftase | FGTI-2734 | FGTI 2734 | KRAS | C-terminal | transferase | tumors | localization | FGTI2734 |
Inhibitors Related | Serotonin hydrochloride | Risedronate Sodium | Risedronic Acid | 3-Methoxybenzamide | Entacapone | Minodronic acid monohydrate | OU749 | Ibandronate sodium | Testosterone propionate | Alendronate sodium hydrate | Flopropione | (E)-Daporinad |
Related Compound Libraries | Bioactive Compound Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |