FTI-277 HCl is an inhibitor of farnesyltransferase (FTase) and a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
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FTI-277, when used at 20 micrometers for 48 hours before irradiation, notably decreases the survival of radioresistant HeLa 3A cells expressing a 24-kDa isoform but does not affect the survival of control HeLa PINA cells. This radiosensitizing effect of FTI-277 is accompanied by an increase in postmitotic cell death in HeLa 3A cells and a decrease in G(2)/M phase arrest in both cell lines[1]. GGTI-298 and FTI-277 treatments hinder migration and invasion of PC-3 cells in both time- and dose-dependent manners[3].
体内研究
FTI-277 therapy prevents the rise in PTP-1B and PTEN protein levels seen in burned mice when compared to the vehicle control. Conversely, FTI-277 doesn't significantly change the expression levels of PTP-1B and PTEN in sham-burned mice[2].
体外研究
FTI-277, when used at 20 micrometers for 48 hours before irradiation, notably decreases the survival of radioresistant HeLa 3A cells expressing a 24-kDa isoform but does not affect the survival of control HeLa PINA cells. This radiosensitizing effect of FTI-277 is accompanied by an increase in postmitotic cell death in HeLa 3A cells and a decrease in G(2)/M phase arrest in both cell lines[1].
GGTI-298 and FTI-277 treatments hinder migration and invasion of PC-3 cells in both time- and dose-dependent manners[3].
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