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FGTI-2734 mesylate
CAS No. : 2702297-24-1
MCE 国际站：FGTI-2734 mesylate
产品活性：FGTI-2734 mesylate 是 RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT) 抑制剂，对 FT 和 GGT 的 IC50s 分别为 250 nM 和 520 nM。FGTI-2734 mesylate 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。
研究领域：Metabolic Enzyme/Protease
作用靶点：Farnesyl Transferase
In Vitro: FGTI-2734 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells.
?FGTI-2734 mesylate (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.
In Vivo: FGTI-2734 mesylate (intraperitoneally; 100 mg/kg/day 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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