683808-78-8

683808-78-8 structure

Name: Poloppin
Chemical Name: 3-{5-(4-Bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrol-2-yl}propanoic acid
CAS Number: 683808-78-8
Molecular Formula: C₂₀H₁₅BrF₃NO₂
Molecular Weight: 438.238
Create Date: 2020-01-11 18:55:21
Modify Date: 2024-09-17 08:24:41
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.

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

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)