Poloppin

Modify Date: 2024-09-17 08:24:41

Poloppin Structure
Poloppin structure
Common Name Poloppin
CAS Number 683808-78-8 Molecular Weight 438.238
Density 1.5±0.1 g/cm3 Boiling Point 536.7±50.0 °C at 760 mmHg
Molecular Formula C20H15BrF3NO2 Melting Point N/A
MSDS N/A Flash Point 278.4±30.1 °C

 Use of Poloppin


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.

 Names

Name 3-{5-(4-Bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrol-2-yl}propanoic acid
Synonym More Synonyms

 Poloppin 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

 Synonyms

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]-