FGTI-2734 |
| Catalog No.GC36038 |
FGTI-2734는 FT 및 GGT-1에 대해 각각 250nM 및 520nM의 IC50을 갖는 RAS C-말단 모방 이중 파르네실 전이효소(FT) 및 게라닐게라닐 전이효소-1(GGT-1) 억제제입니다. FGTI-2734는 KRAS의 막 국소화를 방지할 수 있으므로 KRAS 내성 문제를 해결하고 돌연변이 KRAS 환자 유래 췌장 종양을 저지할 수 있습니다.
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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