FGTI-2734 是 有效的Ras C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT-1) 抑制剂，IC50s 分别为 250 nM 和 520 nM。 它可以阻断 KRas 的膜定位，从而解决 KRas 耐药性问题，并抑制突变的 KRas 胰腺肿瘤。

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.

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.

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.

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C26H31FN6O2S

510.63

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