FTI-2153

FTI-2153

中文名称FTI-2153
中文同义词化合物 T15353;化合物 FTI-2153
英文名称FTI-2153
英文同义词FTI-2153;L-Methionine, N-[[5-[[(1H-imidazol-5-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester;L-Methionine,N-[[5-[[(1H-imidazol-4-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester;FTI2153,FTI 2153
CAS号344900-92-1
分子式C25H30N4O3S
分子量466.6
EINECS号
相关类别
Mol文件344900-92-1.mol
结构式FTI-2153 结构式

FTI-2153 性质

沸点700.1±60.0 °C(Predicted)
密度1.210±0.06 g/cm3(Predicted)
储存条件Store at -20°C
溶解度二甲基亚砜:100 mg/mL(214.32 mM)
酸度系数(pKa)13.00±0.46(Predicted)
形态固体
颜色米白色至浅黄色

FTI-2153 用途与合成方法

FTI-2153 是一种有效、高度选择性的法尼基转移酶 farnesyltransferase (FTase) 抑制剂,IC50 为 1.4 nM。FTI-2153 有效抑制 H-Ras 蛋白的加工修饰,IC50 值为 10 nM,是对其抑制活性是对 Rap1A 蛋白加工的 3000 多倍。

FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status in two human lung cancer cell lines.
FTI-2153 increases the percentage of prometaphase cells with ring-like DNA morphology in transformed and non-transformed cells.
FTI-2153 (15 μM) inhibits T-24 and Calu-1 cell growth by 38 and 36%, respectively. NIH3T3, HFF and HT-1080 are less sensitive and are inhibited by only 8, 8 and 13%, respectively. A-549 and OVCAR3 cell growth is inhibited by 25 and 22%, respectively. Thus, even though T-24 and Calu-1 cells are equisensitive to FTI-2153 cell growth inhibition, FTI-2153 inhibits bipolar spindle formation only in Calu-1 cells. HFF and NIH3T3 cells are both resistant to FTI2153 growth inhibition, yet only NIH3T3 cells are resistant to FTI-2153 inhibition of bipolar spindle formation.

Cell Viability Assay

Cell Line: NIH3T3, HFF, HT1080, T-24, OVCAR3, A-549 and Calu-1 CELLS.
Concentration: 48 h.
Incubation Time: 15 μM.
Result: When A-549 cells were treated with FTI-2153 (15 μM for 48 h), the proportion of cells at prometaphase increased relative to the other phases of mitosis.
FTI-2153 accumulated cells at prometaphase with a rosette-like morphology where chromosomes form a ring surrounding a monoaster of microtubules.
In all cells, except for T-24 and NIH3T3, FTI-2153 treatment increased the proportion of mitotic cells in prometaphase and decreased the percentage of cells in telophase/cytokinesis.
In HT1080 cells, the percentage of cells in prometaphase and telophase/ cytokinesis were 5 and 85% in control cells and 55 and 35% in Treated cells, respectively. Similarly results were also found in HFF cells. Calu-1 and A-549 cells, as described previously, had similarly large changes, whereas OVCAR3 had smaller changes. In contrast, FTI-2153 did not significantly affect the distribution of the different phases of mitosis in T-24 and NIH3T3 cells.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2026/09/15HY-123242FTI-2153344900-92-11 mg2045元
2026/09/15HY-123242FTI-2153
FTI-2153
344900-92-15mg4500元
"FTI-2153"相关产品信息
手霉素A 阿仑膦酸钠三水合物 YM-53601 洛那法尼 米诺磷酸
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