FTI-2148
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- CAS号:
- 251577-09-0
- 英文名:
- FTI-2148
- 英文别名:
- FTI-2148;FTI2148,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]-
- 中文名:
- FTI-2148
- 中文别名:
- 化合物 T11330L
- CBNumber:
- CB32731060
- 分子式:
- C24H28N4O3S
- 分子量:
- 452.57
- MOL File:
- 251577-09-0.mol
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FTI-2148化学性质
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沸点:
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730.1±60.0 °C(Predicted)
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密度:
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1.256±0.06 g/cm3(Predicted)
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溶解度:
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DMSO:0.0(Max Conc. mg/mL);0.0(Max Conc. mM)
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酸度系数(pKa):
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3.49±0.10(Predicted)
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FTI-2148性质、用途与生产工艺
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。
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
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Cell Line:
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KRAS HRAS, and NRAS-transformed NIH3T3 cells
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Concentration:
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30 μM
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Incubation Time:
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Result:
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Inhibited the prenylation of KRAS and NRAS.
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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.
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Animal Model:
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Ras transgenic mouse model
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Dosage:
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100 mg/kg/day
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Administration:
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Subcutaneous injection; 100 mg/kg/day; 14 days
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Result:
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Induced regression by 87 ± 3% of mammary carcinomas in mice.
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FTI-2148
上下游产品信息
上游原料
下游产品
251577-09-0, FTI-2148 相关搜索:
- APIS
- 化合物 T11330L
- 251577-09-0
- FTI2148,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]-
- FTI-2148