XK 469 (XK469)

04/01/2002 - "Previous studies have indicated that XK469 is an antiproliferative agent with a low cytotoxic effect in human H116 tumor cells. "
01/01/2016 - "Our findings suggest that GAS2 could have potential clinical applications for predicting early CRC relapse after radical resection, and that XK469 might impair tumor cell division by reducing GAS2 expression or blocking its cellular translocation. "
07/04/2002 - "These results indicate that the induction of apoptosis by XK469 may account for its anti-tumor activity and such activity is required for the activation of the mitochondrial pathway. "
07/04/2002 - "Here we investigate the ability of XK469 to induce apoptosis of human cancer cells. "
02/01/2002 - "No case of collateral sensitivity was observed; i.e., no agent was markedly more active against the resistant subline L1210/XK-469 than against the parent tumor in mice."

01/01/2011 - "This report describes a 14-year old with relapsed neuroblastoma who experienced disease stabilization for 14 months while receiving (R+)XK469 monotherapy. "
01/01/2011 - "These preclinical results, coupled with the favorable clinical response, demonstrate that (R+)XK469 and similar anti-tumor agents may be effective in the treatment of high-risk neuroblastoma and warrant further testing."
01/01/2011 - "(R+)XK469 inhibited proliferation, caused G(2) cell cycle arrest of neuroblastoma cells in vitro, and inhibited growth of neuroblastoma xenograft tumors. "
01/01/2011 - "The quinoxaline anti-tumor agent (R+)XK469 inhibits neuroblastoma tumor growth."

12/01/2003 - "We have previously reported that XK469 inhibited topoisomerase (topo) IIbeta, in Waldenstrom's macroglobulinemia cell line (WSU-WM) however the inhibition alone is not sufficient to induce apoptosis. "
12/01/2003 - "XK469, a topo IIbeta inhibitor, induces apoptosis in Waldenstrom's macroglobulinemia through multiple pathways."
12/01/2002 - "2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]-propionic acid (XK469) inhibition of topoisomerase IIbeta is not sufficient for therapeutic response in human Waldenstrom's macroglobulinemia xenograft model."
12/01/2002 - "Using the Waldenstrom's macroglobulinemia (WM) cell line WSU-WM, we show that XK469 induced the expression of Topo IIalpha protein by 24 h compared with control. "
12/01/2002 - "In this study, we investigated Topo IIbeta as a target for 2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]-propionic acid (XK469), a novel synthetic quinoxaline phenoxypropionic acid derivative, in a Waldenstrom's macroglobulinemia (WM) model. "

04/01/2002 - "The antiproliferative activity of XK469 was tested using human U-937 leukemia cells in culture. "
10/12/1999 - "Preferential targeting of topoisomerase IIbeta may explain the solid tumor selectivity of XK469 and its analogs because solid tumors, unlike leukemias, often have large populations of cells in the G(1)/G(0) phases of the cell cycle in which topoisomerase IIbeta is high whereas topoisomerase IIalpha, the primary target of many leukemia selective drugs, is low."
04/01/2002 - "Our findings suggest that the antiproliferative effect of XK469 is mediated by inhibiting the MEK/MAPK signaling pathways in U-937 human leukemia cells."
02/01/2002 - "This leukemia subline (L1210/XK469) had reduced sensitivity to VP-16 (with a 4.0 log kill in i.v. implanted L1210/XK469 compared to an 8.0 log kill against i.v. implanted L1210/0). "
01/01/1999 - "In vitro, XK469 demonstrated selective cytotoxicity for several murine solid tumors including colorectal and mammary adenocarcinoma cell lines, when compared to both leukemia and normal epithelial cells. "

01/01/2007 - "The role of autophagy in the death of L1210 leukemia cells initiated by the new antitumor agents, XK469 and SH80."
07/26/2001 - "Using murine leukemia L1210 cells in culture, we found the chiral R(+) form of XK469 to be substantially more cytotoxic than the S(-) form, while the herbicide analog 'Assure' was essentially inactive. "