FTI-2153

生物活性体外研究 FTI-2153 试剂级价格

FTI-2153

CAS号:344900-92-1
英文名:FTI-2153
中文名:FTI-2153
CBNumber:CB62731061
分子式:C25H30N4O3S
分子量:466.6
MOL File:344900-92-1.mol

FTI-2153化学性质

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 :DMSO: 100 mg/mL (214.32 mM)
酸度系数(pKa) :13.00±0.46(Predicted)
形态 :Solid
颜色 :Off-white to light yellow

FTI-2153性质、用途与生产工艺

生物活性 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。

体外研究

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.