FGTI-2734

Research use only, not for human use.

FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.?

FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.?FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively.(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 (100 mg/kg/daily for 18 to 25 days; i.p.) only inhibited tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors.

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Metabolic Enzyme/Protease

Transferase

NMDA receptor

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1247018-19-4

510.6

C26H31FN6O2S

>98% (HPLC)

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Cn1cncc1CN(CCN(CC1CCCCC1)S(=O)(=O)c1ccccn1)c1ccc(cc1F)C#N

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(-20℃)

With Ice Pack

≥ 2 years