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
- 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。
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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.
- 更新日期：2024/11/08
- 产品编号：HY-123242
- 产品名称：FTI-2153
- CAS编号：
- 包装：1 mg
- 价格：2045元
- 更新日期：2024/11/08
- 产品编号：HY-123242
- 产品名称：FTI-2153 FTI-2153
- CAS编号：344900-92-1
- 包装：5mg
- 价格：4500元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：32165
- 优势度：58
- 公司名称：TargetMol Chemicals Inc.
- 联系电话： +8613564774135
- 电子邮件：zijue.cai@tsbiochem.com
- 国家：美国
- 产品数：19885
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：52924
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
