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FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 3,010 | 期货 | |
10 mg | ¥ 5,560 | 期货 | |
50 mg | ¥ 17,035 | 期货 | |
100 mg | ¥ 29,785 | 期货 | |
200 mg | 询价 | 期货 | |
500 mg | 询价 | 期货 | |
1 mL x 10 mM (in DMSO) | ¥ 4,005 | 期货 |
产品描述 | FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors. |
靶点活性 | FT:250 nM , GGT:520 nM |
体外活性 | FGTI-2734 mesylate (3-30 μM;?72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 mesylate (1-30 μM; 72 hours) induces apoptosis in mutant KRAS-dependent, but not mutant KRAS- independent, human cancer cells. ??FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells. |
体内活性 | 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. |
别名 | FGTI-2734 mesylate |
分子量 | 606.73 |
分子式 | C27H35FN6O5S2 |
CAS No. | 2702297-24-1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 75 mg/mL (123.61 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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