2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
EMICORON as a novel G-quadruplex (G4) ligand showing high selectivity for G4 structures over the duplex DNA, causing telomere damage and inhibition of cell proliferation in transformed and tumor cells.The antitumoral effect of EMICORON on advanced models of human colon cancer (CRC) that could adequately predict human clinical outcomes.Results showed that EMICORON was well tolerated in mice, as no adverse effects were reported, and a low ratio of sensitivity across human and mouse bone marrow cells was observed, indicating a good potential for reaching similar blood levels in humans. Moreover, EMICORON showed a marked therapeutic efficacy, as it inhibited the growth of patient-derived xenografts (PDXs)and orthotopic CRC, and strongly reduced the dissemination of tumor cells to lymphnodes, intestine, stomach and liver. Finally, activation of DNA damage, impairment of proliferation and angiogenesis are proved to be key determinants of EMICORON antitumoral activity.Performed on advanced experimental models of human CRC that bridge the translational gap between preclinical and clinical studies, demonstrated that EMICORON had an unprecedented antitumor activity warranting further studies of EMICORON-based combination treatments.
