| Identification | Back Directory | [Name]
2-Naphthaleneacetamide, N-(5-cyclopropyl-1H-pyrazol-3-yl)- | [CAS]
326823-27-2 | [Synonyms]
PNU292137
PNU-292137
PNU 292137
2-Naphthaleneacetamide, N-(5-cyclopropyl-1H-pyrazol-3-yl)- | [Molecular Formula]
C18H17N3O | [MOL File]
326823-27-2.mol | [Molecular Weight]
291.35 |
| Hazard Information | Back Directory | [Uses]
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model[1]. | [IC 50]
CDK2/cyclinA: 37 nM (IC50); CDK2/cyclin E: 92 nM (IC50); Cdk5/p25: 114 nM (IC50); CDK1/cyclinB: 270 nM (IC50); CDK4/cyclinD1: >10000 nM (IC50); GSK-3β: 1905 nM (IC50); ERK-2: 4600 nM (IC50) | [References]
[1] Paolo Pevarello, et al. 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. J Med Chem. 2004 Jun 17;47(13):3367-80. DOI:10.1021/jm031145u |
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