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Chemical Structure : NMS-P937
CAS No.: 1034616-18-6
Catalog No.: PC-22312Not For Human Use, Lab Use Only.
NMS-P937 (Onvansertib, NMS-1286937) is a potent, selective and orally available PLK1 inhibitor with IC50 of 2 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $118 | In stock | |
| 50 mg | $248 | In stock | |
| 100 mg | Get quote | ||
| 250 mg | Get quote |
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NMS-P937 (Onvansertib, NMS-1286937) is a potent, selective and orally available PLK1 inhibitor with IC50 of 2 nM, >300-fold selective over PLK2/3.
NMS-P937 exhibits antiproliferative effect on A2780 cells with IC50 of 42 nM.
NMS-P937 potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits xenograft tumor growth with clear PLK1-related mechanism of action at well-tolerated doses in mice after oral administration.
NMS-P937 shows potential for combination in clinical settings with approved cytotoxic drugs, causing tumor regression in HT29 human colon adenocarcinoma xenografts upon combination with irinotecan and prolonged survival of animals in a disseminated model of acute myelogenous leukemia in combination with cytarabine.
| M.Wt | 532.53 | |
| Formula | C24H27F3N8O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(2-Hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide |
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1. Beria I, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74.
2. Valsasina B, et al. Mol Cancer Ther. 2012 Apr;11(4):1006-16.
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