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编 号：F718693
分子式：C28H30F6N4O7S
分子量：680.62
分子式：C28H30F6N4O7S
分子量：680.62
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CAS No: 817586-01-9
产品详情
生物活性：
FTI-2148 diTFA is a RAS C-terminal mimetic dual?farnesyl transferase (FT-1)?and?geranylgeranyl transferase-1 (GGT-1)?inhibitor with?IC50s of 1.4 nM and 1.7 μM, respectively.
体内研究：
FTI-2148 (intraperitoneal?injection; 25 or 50 mpk/day with a mini-pump; started on day 15 andstopped 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) inhibitstumor 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:Reduced regression by 87 ± 3% of mammary carcinomas in mice.
体外研究：
FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells.FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I.
FTI-2148 diTFA is a RAS C-terminal mimetic dual?farnesyl transferase (FT-1)?and?geranylgeranyl transferase-1 (GGT-1)?inhibitor with?IC50s of 1.4 nM and 1.7 μM, respectively.
体内研究：
FTI-2148 (intraperitoneal?injection; 25 or 50 mpk/day with a mini-pump; started on day 15 andstopped 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) inhibitstumor 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:Reduced regression by 87 ± 3% of mammary carcinomas in mice.
体外研究：
FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells.FTI-2148 diTFA is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I.
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