FGTI-2734 |
| Katalog-Nr.GC36038 |
FGTI-2734 ist ein C-terminal mimetischer RAS-Hemmer mit dualer Farnesyltransferase (FT) und Geranylgeranyltransferase-1 (GGT-1) mit IC50-Werten von 250 nM und 520 nM fÜr FT bzw. GGT-1. FGTI-2734 kann die Membranlokalisierung von KRAS verhindern, wodurch das Problem der KRAS-Resistenz gelÖst und mutierte KRAS-Patienten-abgeleitete BauchspeicheldrÜsentumoren vereitelt werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1247018-19-4
Sample solution is provided at 25 µL, 10mM.
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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]. IC50: 250 nM (FT) and 520 nM (GGT)[1]
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
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]
[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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