FTI-2153
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- CAS号:
- 344900-92-1
- 英文名:
- FTI-2153
- 英文别名:
- FTI-2153;FTI2153,FTI 2153;L-Methionine,N-[[5-[[(1H-imidazol-4-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester;L-Methionine, N-[[5-[[(1H-imidazol-5-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
- 中文名:
- FTI-2153
- 中文别名:
- 化合物 T15353
- CBNumber:
- CB62731061
- 分子式:
- C25H30N4O3S
- 分子量:
- 466.6
- MOL File:
- 344900-92-1.mol
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FTI-2153化学性质
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沸点:
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700.1±60.0 °C(Predicted)
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密度:
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1.210±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 100 mg/mL (214.32 mM)
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酸度系数(pKa):
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13.00±0.46(Predicted)
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FTI-2153性质、用途与生产工艺
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
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Cell Line:
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NIH3T3, HFF, HT1080, T-24, OVCAR3, A-549 and Calu-1 CELLS.
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Concentration:
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48 h.
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Incubation Time:
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15 μM.
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Result:
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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.
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FTI-2153
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-123242 | FTI-2153 | | 1 mg | 2045元 |
| 2024/04/30 | HY-123242 | FTI-2153
FTI-2153 | 344900-92-1 | 5mg | 4500元 |
344900-92-1, FTI-2153 相关搜索:
- 抑制剂
- 化合物 T15353
- 344900-92-1
- FTI2153,FTI 2153
- L-Methionine,N-[[5-[[(1H-imidazol-4-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
- L-Methionine, N-[[5-[[(1H-imidazol-5-ylmethyl)amino]methyl]-2'-methyl[1,1'-biphenyl]-2-yl]carbonyl]-, methyl ester
- FTI-2153