Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apopt
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Serine/threonine-protein kinase PLK1 inhibitor
Product Description
Information
Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selectivePolo-like Kinase 1 (PLK1)inhibitor withIC50of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed byapoptosisin cancer cell lines and inhibits tumor growth. Phase 1.
Targets
PLK1 2 nM
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.
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.
Cell Research(from reference)
Cell lines：137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomas
1.Beria I, Bossi RT, Brasca MG, Caruso M, Ceccarelli W, Fachin G, Fasolini M, Forte B, Fiorentini F, Pesenti E et al.. (2011) 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, 21 (10):(2969-74). [PMID:21470862]
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H2202402