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 |
Canonical SMILES | CSCC[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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |