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FTI-2153 TFA

CAS No. :

MCE 站：FTI-2153 TFA

产品活性：FTI-2153 TFA 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 TFA 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。

研究领域：Metabolic Enzyme/Protease

作用靶点：Farnesyl Transferase

In Vitro: 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.

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