FGTI-2734

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FGTI-2734 可以阻止 KRAS 的膜定位，从而解决 KRAS 耐药问题并阻止突变 KRAS 患者来源的胰腺肿瘤。

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.(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.

FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells. 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. Apoptosis Analysis Cell Line:MiaPaCa2, L3.6pl and Calu6 cells Concentration:1, 3, 10, 30 μM Incubation Time:72 hours Result:Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.Western Blot Analysis Cell Line:KRAS, HRAS, and NRAS-transformed NIH3T3 cells Concentration:3, 10, 30 μM Incubation Time:72 hours Result:Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.

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. Animal Model:Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells.Dosage:100 mg/kg Administration:Intraperitoneally; daily; for 18 to 25 days Result:Inhibited tumor growth in mutant KRAS-dependent tumors.

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Metabolic Enzyme/Protease

Transferase

NMDA receptor

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1247018-19-4

510.63

C26H31FN6O2S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (97.92 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years