| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+90% Corn Oil : 5 mg/mL (9.79 mM), Sonication is recommended. DMSO : 50 mg/mL (97.92 mM), Sonication is recommended.
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| Keywords | tumors | transferase | patient-derived | pancreatic | mimetic | membrane | localization | KRAS | Inhibitor | inhibit | GGTase I | GGT-1 | geranylgeranyl | Ftase | FT | FGTI-2734 | FGTI2734 | FGTI 2734 | Farnesyl transferase (FTase) | Farnesyl Transferase | farnesyl | C-terminal |
| Inhibitors Related | Adagrasib | Serotonin hydrochloride | RMC-9805 | D(+)-Raffinose pentahydrate | (R)-Naproxen | Ketoconazole | MRTX1133 | Risedronic Acid | Entacapone | Sotorasib | Daraxonrasib | Flopropione |
| Related Compound Libraries | Bioactive Compound Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Metabolism Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Covalent Inhibitor Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | MAPK Inhibitor Library |