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344900-92-1

中文名稱 FTI-2153
英文名稱 FTI-2153
CAS 344900-92-1
分子式 C25H30N4O3S
分子量 466.6
MOL 文件 344900-92-1.mol
344900-92-1 結(jié)構(gòu)式 344900-92-1 結(jié)構(gòu)式

基本信息

中文別名
化合物 T15353
英文別名
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

物理化學(xué)性質(zhì)

沸點(diǎn)700.1±60.0 °C(Predicted)
密度1.210±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 100 mg/mL (214.32 mM)
酸度系數(shù)(pKa)13.00±0.46(Predicted)
形態(tài)Solid
顏色Off-white to light yellow

常見問題列表

生物活性
FTI-2153 是一種有效、高度選擇性的法尼基轉(zhuǎn)移酶 farnesyltransferase (FTase) 抑制劑,IC50 為 1.4 nM。FTI-2153 有效抑制 H-Ras 蛋白的加工修飾,IC50 值為 10 nM,是對其抑制活性是對 Rap1A 蛋白加工的 3000 多倍。
體外研究

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.
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