LKT Labs

Biochemicals for Life Science Research

NMS-1286937

NMS-1286937

Product ID N5072
Cas No. 1034616-18-6
Purity ≥98%
Product Unit SizeCostQuantityStock
1 mg $104.80 In stock
5 mg $167.30 In stock
10 mg $254.00 Please Inquire
Bulk Quote

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Description

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.

Product Info

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
Solubility

DMSO 42 mg/mL warmed (78.87 mM) Ethanol 10 mg/mL warmed (18.77 mM) Water Insoluble
Appearance

White to off white powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

N5072 MSDS PDF
Info Sheet

N5072 Info Sheet PDF

References

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.

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