Molecular Weight(MW): 532.52
NMS-P937 (NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Phase 1.
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|Description||NMS-P937 (NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Phase 1.|
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. 
|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.  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. |
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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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.
|In vitro||DMSO||42 mg/mL warmed (78.87 mM)|
|Ethanol||10 mg/mL warmed (18.77 mM)|
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