FTI-2148
- CAS号:251577-09-0
- 英文名:FTI-2148
- 中文名:FTI-2148
- CBNumber:CB32731060
- 分子式:C24H28N4O3S
- 分子量:452.57
- MOL File:251577-09-0.mol
- 沸点 :730.1±60.0 °C(Predicted)
- 密度 :1.256±0.06 g/cm3(Predicted)
- 溶解度 :DMSO:0.0(Max Conc. mg/mL);0.0(Max Conc. mM)
- 酸度系数(pKa) :3.49±0.10(Predicted)
FTI-2148性质、用途与生产工艺
- 生物活性 FTI-2148 是 RAS C 末端修饰的法呢基转移酶 (FT-1) 香叶基转移酶1 (GGT-1) 的抑制剂，抑制 FT-1 和 GGT-1 的 IC50 分别为 1.4 nM 和 1.7 μM。
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靶点
IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)
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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 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. -
体内研究
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.
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