Name | FTI-2148 |
Synonyms | FTI-2148 N-[5-(1H-Imidazol-4-ylmethylaminomethyl)-2'-methylbiphenyl-2-ylcarbonyl]-L-methionine L-Methionine, N-[[5-[[(1H-imidazol-5-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]- |
CAS | 251577-09-0 |
Molecular Formula | C24H28N4O3S |
Molar Mass | 452.57 |
Density | 1.256±0.06 g/cm3(Predicted) |
Boling Point | 730.1±60.0 °C(Predicted) |
pKa | 3.49±0.10(Predicted) |
Storage Condition | -20°C,干燥,密封 |
MDL | MFCD08056245 |
biological activity | FTI-2148 is the C- terminal modified farnesyl transferase (FT-1) of RAS the IC50 of the inhibitor of geranyl transferase 1 (GGT-1) for inhibition of FT-1 and GGT-1 were 1.4 nM and 1.7 μm, respectively. |
Target | IC50: 1.4 nM (FT-1); 1.7 μm (GGT-1) |
Cell Line: | KRAS HRAS, and NRAS-transformed NIH3T3 cells |
Concentration: | 30 μM |
Incubation Time: | |
Result: | Inhibited the prenylation of KRAS and NRAS. Induced regression by 87 ± 3% of mammary carcinomas in mice. |
Animal Model: | Rastransgenic mouse model |
Dosage: | 100 mg/kg/day |
Administration: | Subcutaneousinjection; 100 mg/kg/day; 14 days |