CAS NO: | 251577-09-0 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
生物活性 | FTI-2148 is aRASC-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[1]. | ||||||||
IC50& Target | IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1] | ||||||||
体外研究 (In Vitro) | FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1].FTI-2148 is againstP. falciparumPFT, Mammalian PFT and Mammalian PGGT-I with IC50values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I[2]. Western Blot Analysis[]
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体内研究 (In Vivo) | 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[1].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[1].FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[1].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[3].
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分子量 | 452.57 | ||||||||
Formula | C24H28N4O3S | ||||||||
CAS 号 | 251577-09-0 | ||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |