FGTI-2734 是 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，对 FT 和 GGT-1 的IC50s 分别为 250 nM 和 520 nM。 FGTI-2734 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。
| 生物活性 | FGTI-2734 is aRASC-terminal mimetic dualfarnesyl transferase(FT)andgeranylgeranyl transferase-1 (GGT-1)inhibitor withIC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1]. |
| IC50& Target | IC50: 250 nM (FT) and 520 nM (GGT-1)[1] |
体外研究
(In Vitro) | 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 | | 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[1] | 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. |
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体内研究
(In Vivo) | 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] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(97.92 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9584 mL | 9.7918 mL | 19.5837 mL | | 5 mM | 0.3917 mL | 1.9584 mL | 3.9167 mL | | 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 7.5 mg/mL (14.69 mM); Clear solution
此方案可获得 ≥ 7.5 mg/mL (14.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
