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FTI-2153 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FTI-2153 TFA图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
FTI-2153TFA是一种有效、高度选择性的法尼基转移酶farnesyltransferase(FTase)抑制剂,IC50为1.4nM。FTI-2153TFA有效抑制H-Ras蛋白的加工修饰,IC50值为10nM,是对其抑制活性是对Rap1A蛋白加工的3000多倍。
Canonical SMILESCSCC[C@@H](C(OC)=O)NC(C1=CC=C(CNCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O.OC(C(F)(F)F)=O
分子式C27H31F3N4O5S
分子量580.62
溶解度DMSO: 90 mg/mL (155.01 mM)
储存条件-20℃, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity[1].

FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status in two human lung cancer cell lines[2].FTI-2153 increases the percentage of prometaphase cells with ring-like DNA morphology in transformed and non-transformed cells[2].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[2]. Cell Viability Assay[2] Cell Line: NIH3T3, HFF, HT1080, T-24, OVCAR3, A-549 and Calu-1 CELLS.

[1]. Sun J, et al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26. [2]. N C Crespo, et al. The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status. Cell Death Differ. 2002 Jul;9(7):702-9.