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Cell Cycle/Checkpoint PLK NMS-P937

NMS-P937

Catalog No. T6247   CAS 1034616-18-6
Synonyms: NMS-1286937, NMS-1286937

NMS-P937 (NMS1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher over PLK2/PLK3.

NMS-P937, CAS 1034616-18-6
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 80.00
10 mg In stock 112.00
25 mg In stock 202.00
50 mg In stock 290.00
100 mg In stock 490.00
200 mg In stock 873.00
1 mL * 10 mM (in DMSO) In stock 90.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NMS-P937 (NMS1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher over PLK2/PLK3.
Targets&IC50 PLK1 : ic50 2nM,   PLK2 : ic50 >10μM,   PLK3 : ic50 >10μM,  
In vitro NMS-P937 shows a broad-spectrum antiproliferative activity against different solid tumor, leukemias and lymphomas cell lines. NMS-P937 potently causes a mitotic cell-cycle arrest followed by apoptosis in A2780 cells. [2]
In vivo In mice xenografted with human HCT116 colon adenocarcinoma cells, NMS-P937 (90 mg/kg/d i.v. or p.o.) shows a significant tumor growth inhibition. [1] In mice bearing HT29, Colo205 colorectal, or A2780 ovarian xenograft tumors, NMS-P937 inhibits xenograft tumor growth. In addition, NMS-P937, in combination with approved cytotoxic drugs, causes enhanced tumor regression, and prolongs survival of animals. [2]
Kinase Assay Kinase profile: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein substrates are trans-phosphorylated by their specific serine-threonine or tyrosine kinase, in the presence of ATP traced with 33P-γ-ATP, at optimized buffer and cofactors conditions. At the end of the phosphorylation reaction, more than 98% unlabeled ATP and radioactive ATP is captured by adding an excess of the ion exchange dowex resin; the resin then settles down to the bottom of the reaction plate by gravity. Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting. Inhibitory potency evaluation for all the tested kinases was performed at 25 °C using a 60 min end-point assay where the concentrations of ATP and substrates are kept equal to 2 x αKm and saturated (>5 x αKm), respectively.
Cell Research
Cells are seeded into 96- or 384-well plates at densities ranging from 10,000 to 30,000/cm2 for adherent and 100,000/mL for nonadherent cells in appropriate medium supplemented with 10% fetal calf serum. After 24 hours, cells were treated in duplicate with serial dilutions of NMS-P937, and 72 hours later, the viable cell number was assessed by the CellTiter-Glo Assay (Promega). IC50 values were calculated with a sigmoidal fitting algorithm (Assay Explorer MDL). Experiments were carried out independently at least twice.(Only for Reference)
Cell lines: 137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomas
Synonyms NMS-1286937 , NMS-1286937
Purity 99.76%
Molecular Weight 532.52
Formula C24H27F3N8O3
CAS No. 1034616-18-6

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 39 mg/mL (73.2 mM)

Ethanol: 10 mg/mL (18.77 mM), warmed

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Beria I, et al. Bioorg Med Chem Lett. 2011, 21(10), 2969-2974. 2. Valsasina B, et al. Mol Cancer Ther. 2012, 11(4), 12006-12016.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library DNA Damage & Repair Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Fluorochemical Library Cell cycle related Compound Library

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