ispinesib

11/01/2021 - "In the PDX mouse model, ispinesib dramatically reduced tumor growth relative to vehicle control (652.2 mm3 vs 18.1 mm3 in mean tumor volume, P < .01 by ANOVA; 545 mg vs 28 mg in tumor weight, P < .01, by ANOVA). "
06/18/2008 - "Ispinesib (SB-715992), a potent and selective inhibitor of KSP, is currently in phase II clinical trials for the treatment of multiple tumor types. "
09/12/2023 - "We generated patient-derived xenografts to show that ispinesib-resistant cells form less aggressive tumors in vivo, even in the absence of drug. "
06/13/2023 - "In vivo, we validated that ispinesib increased the fraction of tumor cells arrested in mitosis as well as increased apoptosis. "
01/01/2021 - "Ispinesib, a KIF11-inhibitor, effectively inhibited tumor proliferation in all seven cell lines. "

09/01/2008 - "Ispinesib was inactive in this study of patients with androgen-independent, and largely docetaxelresistant, prostate cancer. "
01/24/2006 - "Hence, we believe that SB715992 could be a novel agent for the treatment of prostate cancer with greater success when combined with a non-toxic natural agent like genistein."
01/24/2006 - "Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line."
09/01/2008 - "Southwest Oncology Group phase II study of ispinesib in androgen-independent prostate cancer previously treated with taxanes."
01/24/2006 - "Our major objective was a) to investigate the cell growth inhibitory effects of SB715992 on PC-3 human prostate cancer cell line, b) to investigate whether the growth inhibitory effects of SB715992 could be enhanced when combined with genistein, a naturally occurring isoflavone and, c) to determine gene expression profile to establish molecular mechanism of action of SB715992. "

06/01/2008 - "A phase II study was conducted to examine the efficacy of ispinesib in recurrent or metastatic head and neck squamous cell carcinoma (RMHNSC). "
06/01/2008 - "Phase II study of ispinesib in recurrent or metastatic squamous cell carcinoma of the head and neck."
04/15/2013 - "Furthermore, growth of HNSCC cells engrafted in immunodeficient mice was significantly inhibited after ispinesib treatment. "
04/15/2013 - "We showed that ispinesib induces a G2 arrest, causes aberrant chromosome segregation, and induces cell death in HNSCC in vitro, whereas primary keratinocytes are less sensitive. "

12/15/2009 - "Ispinesib was highly potent against the PPTP's in vitro cell lines with a median IC(50) of 4.1 nM. Ispinesib (10 mg/kg) induced unexplained toxicity in mice bearing osteosarcoma xenografts and exceeded the MTD in 12 of 40 non-osteosarcoma xenografts. "

11/01/2021 - "Ispinesib, identified by inhibitor library screening, could be a promising novel therapeutic agent for pancreatic cancer. "
11/01/2021 - "The expression of its target Eg5 is associated with poorer postoperative prognosis and is important for the clinical efficacy of ispinesib in pancreatic cancer."
11/01/2021 - "The clinical significance of the expression of the ispinesib target Eg5 was investigated in 165 pancreatic cancer patients by immunohistochemical staining and in Eg5-positive pancreatic cancer patient-derived xenograft (PDX) mouse models. "
11/01/2021 - "Ispinesib was found to mediate effective antitumor effects in pancreatic cancer. "
11/01/2021 - "In this manner, we identified ispinesib as a candidate and attempted to determine its clinical efficacy and the biological significance of its functional target Eg5 in pancreatic cancer. "