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编 号：F425800
分子式：C20H15BrF3NO2
分子量：438.24
分子式：C20H15BrF3NO2
分子量：438.24
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CAS No: 683808-78-8
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生物活性：
Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9?μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5?μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis.?Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
体外研究：
Poloppin (0-200 μM) competitively inhibits the binding of a?TAMRA-labeled substrate peptide to the PLK1 PBD, exhibiting an IC50 value of 26.9?μM in an FP assay; the isothermal titration calorimetry of Poloppin binding to the PBD domain of PLK1 with a Kd of 29.5?μM.Poloppin (0-100 μM) triggers a dose-dependent mitotic arrest and induces multiple anomalies in?mitosis in cells, the EC50 value is 29.9?μM. In representative images of U2OS cells with 12.5?μM Poloppin, Poloppin 相关抗体:Cell Viability AssayCell Line:SW48 isogenic parental or KRAS G12D?cells
Concentration:0-200 μM
Incubation Time:24 hours
Result:Inhibited cell growth expressing mutant KRAS in two-dimensional and organoid Cultures.
Cell Cytotoxicity AssayCell Line:SW48 isogenic parental or KRAS G12D?cells
Concentration:0-200 μM
Incubation Time:24 hours
Result:Selectively increased sensitization of mutant KRAS-expressing cells to inhibitors of the c-MET tyrosine kinase.
Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9?μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5?μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis.?Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
体外研究：
Poloppin (0-200 μM) competitively inhibits the binding of a?TAMRA-labeled substrate peptide to the PLK1 PBD, exhibiting an IC50 value of 26.9?μM in an FP assay; the isothermal titration calorimetry of Poloppin binding to the PBD domain of PLK1 with a Kd of 29.5?μM.Poloppin (0-100 μM) triggers a dose-dependent mitotic arrest and induces multiple anomalies in?mitosis in cells, the EC50 value is 29.9?μM. In representative images of U2OS cells with 12.5?μM Poloppin, Poloppin 相关抗体:Cell Viability AssayCell Line:SW48 isogenic parental or KRAS G12D?cells
Concentration:0-200 μM
Incubation Time:24 hours
Result:Inhibited cell growth expressing mutant KRAS in two-dimensional and organoid Cultures.
Cell Cytotoxicity AssayCell Line:SW48 isogenic parental or KRAS G12D?cells
Concentration:0-200 μM
Incubation Time:24 hours
Result:Selectively increased sensitization of mutant KRAS-expressing cells to inhibitors of the c-MET tyrosine kinase.
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