NMS-1286937
- Onvansertib - NMS-P 937- Soluble in DMSO
- MF: C24H27F3N8O3
- MW: 532.52
Description
NMS1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. NMS-1286937 selectively and effectively inhibits PLK1 (with IC50 at low nM), inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells.
More Information
| Parent CAS No. | 1034616-18-6 |
|---|---|
| Chemical Name | 1-(2-Hydroxyethyl)-8-(5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(NC2C(OC(F)(F)F)=CC=C(N3CCN(C)CC3)C=2)N=C2C3N(CCO)N=C(C(N)=O)C=3CCC2=CN=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H27F3N8O3/c1-33-6-8-34(9-7-33)15-3-5-18(38-24(25,26)27)17(12-15)30-23-29-13-14-2-4-16-20(22(28)37)32-35(10-11-36)21(16)19(14)31-23/h3,5,12-13,36H,2,4,6-11H2,1H3,(H2,28,37)(H,29,30,31) |
| InChiKey | QHLVBNKYJGBCQJ-UHFFFAOYSA-N |
| CID | 49792852 |
| Short Description | PLK1 inhibitor |
References
- A Casolaro 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.
- B Valsasina 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.
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