251577-09-0
251577-09-0 結(jié)構(gòu)式
基本信息
化合物 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]-
物理化學(xué)性質(zhì)
常見問題列表
IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)
FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells.FTI-2148 is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC 50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I.
Western Blot Analysis []
| Cell Line: | KRAS HRAS, and NRAS-transformed NIH3T3 cells |
| Concentration: | 30 μM |
| Incubation Time: | |
| Result: | Inhibited the prenylation of KRAS and NRAS. |
FTI-2148 (intraperitoneal?injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model. FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model.FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a?ras?transgenic mouse model. FTI-2148 (subcutaneous?injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo?settings.
| Animal Model: | Ras?transgenic mouse model |
| Dosage: | 100 mg/kg/day |
| Administration: | Subcutaneous?injection; 100 mg/kg/day; 14 days |
| Result: | Induced regression by 87 ± 3% of mammary carcinomas in mice. |