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Chemical Structure : Poloppin
Catalog No.: PC-61200Not For Human Use, Lab Use Only.
Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.
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Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.
Poloppin triggers dose-dependent mitotic arrest with non-congressed chromosomes in human cell lines, preferentially kills cells expressing mutant KRAS (SW48 G12D GI50=5.2 uM, SW48 Wt GI50=13.7 uM).
Poloppin sensitizes mutant KRAS-expressing cells to clinical inhibitors of c-MET.
| M.Wt | 438.244 | |
| Formula | C20H15BrF3NO2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Narvaez AJ, et al. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7.
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