Poloppin

Names

[ Name ]:
Poloppin

[Synonym ]:
3-{5-(4-Bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrol-2-yl}propanoic acid
1H-Pyrrole-2-propanoic acid, 5-(4-bromophenyl)-1-[2-(trifluoromethyl)phenyl]-

Biological Activity

[Description]:

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; 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), sensitizes mutant KRAS-expressing cells to clinical inhibitors of c-MET.

[References]

References 1. Narvaez AJ, et al. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7. View Related Products by Target Polo-like Kinase (PLK)

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
536.7±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₀H₁₅BrF₃NO₂

[ Molecular Weight ]:
438.238

[ Flash Point ]:
278.4±30.1 °C

[ Exact Mass ]:
437.023804

[ LogP ]:
6.08

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.582

Related Compounds

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