Toggle Nav

NMS-1286937

In stock
Catalog No.
B4094
PLK1 inhibitor, orally bioavailable
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$210.00
In stock
5mg
$121.00
In stock
10mg
$167.00
In stock
50mg
$361.00
In stock
100mg
$587.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

NMS-1286937 (NMS-P937) is a potent and selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 value of 2 nM [1].

PLK1 is a serine/threonine protein kinase and plays an important role in the cell cycle control machinery. PLK1 is involved in mitotic entry, bipolar mitotic spindle formation, centrosome duplication, transition from metaphase to anaphase, maintenance of genomic stability and cytokinesis [1].

NMS-1286937 is an orally bioavailable PLK1 inhibitor. In cell lines established from solid tumors, leukemias and lymphomas, NMS-P937 inhibited tumor cell proliferation. In A2780 cells, NMS-P937 caused a G2-M cell-cycle block. In the mitotic phase, NMS-P937 induced apoptotic death with misaligned chromosomes and an aberrant number of spindles poles [2]. In human osteosarcoma (OS) cell lines, NMS-P937 inhibited migration and clonogenic ability of cell lines. In ABCB1-overexpressing, Doxorubicin (DX)-resistant cell lines, combination of NMS-P937 and DX reverted DX-resistance by inhibiting ABCB1 transport activity [3].

In Harlan nu/nu mice, NMS-P937 exhibited a good pharmacokinetic profile with low clearance, high AUC and Cmax, and acceptable oral bioavailability. In mice xenografted with human HCT116 colon adenocarcinoma cells, NMS-P937 (45 mg/kg) inhibited tumor growth by 83% and reduced body weight by 16% [1].

References:
[1].  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, 21(10): 2969-2974.
[2].  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, 11(4): 1006-1016.
[3].  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, 32(6): 1167-1180.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt532.52
Cas No.1034616-18-6
FormulaC24H27F3N8O3
Solubility≥13.3mg/mL in DMSO
SDFDownload SDF
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

NMS-1286937