FTI-2153 TFA |
| Catalog No.GC61775 |
FTI-2153 TFA est un inhibiteur puissant et hautement sélectif de la farnésyltransférase (FTase), avec une IC50 de 1,4 nM. FTI-2153 TFA est >3000 fois plus efficace pour bloquer le traitement de H-Ras (IC50, 10 nM) que celui de Rap1A. Activité anticancéreuse.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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.
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