NMS-1286937
NMS-1286937 is an inhibitor of polo-like kinase 1 (PLK1) that is currently in clinical trials as a potential treatment for various cancers; it exhibits anticancer chemotherapeutic activity. In osteosarcoma cells, NMS-1286937 induces cell cycle arrest and apoptosis and inhibits cell growth. In animal models of acute myelogenous leukemia (AML), this compound increases survival time and decreases tumor cell infiltration. Additionally, NMS-1286937 inhibits cell proliferation and induces apoptosis, cell cycle arrest, and tumor regression in cellular and animal models of colon cancer.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18949386
| Cas No. |
1034616-18-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C24H27F3N8O3 |
| Formula Wt. |
532.52 |
| IUPAC Name |
1-(2-Hydroxyethyl)-8-{[5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide |
| Synonym |
NMS1286937, NMS-P937 |
| Appearance |
White to off white powder |
Sero V, Tavanti E, Vella S, et al. Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance. Invest New Drugs. 2014 Dec;32(6):1167-80. PMID: 25193492.
Casolaro A, Golay J, Albanese C, et al. The Polo-Like Kinase 1 (PLK1) inhibitor NMS-P937 is effective in a new model of disseminated primary CD56+ acute monoblastic leukaemia. PLoS One. 2013;8(3):e58424. PMID: 23520509.
Valsasina B, Beria I, Alli C, et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther. 2012 Apr;11(4):1006-16. PMID: 22319201.
Beria I, Bossi RT, Brasca MG, et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74. PMID: 21470862.
