683808-78-8
Chemical Structure
Poloppin
- CAS No.: 683808-78-8
- Formula:C20H15BrF3NO2
- Molecular Weight:438.24
IUPAC Name: 3-(5-(4-bromophenyl)-1-(2-(trifluoromethyl)phenyl)-1H-pyrrol-2-yl)propanoic acid
InChIKey: OCUKOJUZSNFVFQ-UHFFFAOYSA-N
SMILES: O=C(O)CCC1=CC=C(C2=CC=C(Br)C=C2)N1C3=CC=CC=C3C(F)(F)F
Biological Activity: 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[1].
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Poloppin | 99.40% | 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. | ||||||||||||||||||||
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Keywords
