FGTI-2734
规格
| Cas Number | 1247018-19-4 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 50 mg/mL (97.92 mM; Need ultrasonic) |
| 过滤标签 | Farnesyl Transferase,Metabolic Enzyme/Protease |
| 储存温度 | 2-8°C储存 |
| 运输条件 | 冰袋运输 |
| 生化和生理学机理 | FGTI-2734 是一种 RAS C--terminal mimetic 双法尼基转移酶（FT）和香叶基转移酶-1（GGT-1）抑制剂，FT 和 GGT-1 的 IC 50 s 分别为 250 nM 和 520 nM。FGTI-2734 可阻止 KRAS 的膜定位，从而解决 KRAS 的膜定位问题。 |
| 英文描述 |
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC 50 s 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell 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 AnalysisCell 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. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: 250 nM (FT) and 520 nM (GGT-1) |