Onvansertib (NMS-P937)

For research use only.

Catalog No.S7255 Synonyms: PCM-075, NMS1286937

2 publications

Onvansertib (NMS-P937) Chemical Structure

CAS No. 1034616-18-6

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 apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.

Selleck's Onvansertib (NMS-P937) has been cited by 2 publications

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Biological Activity

Description 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 apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.
Targets
PLK1 [1]
()
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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 NGHHbmtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3faSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOsJGlEPTBiPTCwMlA1OiEQvF2u MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR5MEi2Nkc,OjF2N{C4OlI9N2F-
CAL51 MoLHR4VtdCCleXPs[UBie3OjeR?= NX36O41NOC5zIITvJFEhfU1? M3eyflI1KGi{cx?= M{HLeGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGNCVDVzIHPlcIx{KGG2IECuNUB1dyBzIIXNJIFnfGW{IEK0JIhzeyCkeTDmcI94KGO7dH;t[ZRzgQ>? MoX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2N{C4OlIoRjJzNEewPFYzRC:jPh?=

... Click to View More Cell Line Experimental Data
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]

Protocol

Kinase Assay:[1]
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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:[2]
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  • Cell lines: 137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomas
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method: 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)

Solubility (25°C)

In vitro DMSO 42 mg/mL warmed (78.87 mM)
Water Insoluble
Ethanol '10 mg/mL warmed

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 532.52
Formula

C24H27F3N8O3
CAS No. 1034616-18-6
Storage powder
in solvent
Synonyms PCM-075, NMS1286937
Smiles CN1CCN(CC1)C2=CC(=C(C=C2)OC(F)(F)F)NC3=NC=C4CCC5=C(C4=N3)N(N=C5C(=O)N)CCO

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03303339 Active not recruiting Drug: Onvansertib|Drug: Cytarabine|Drug: Decitabine Acute Myeloid Leukemia Cardiff Oncology November 17 2017 Phase 1|Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PLK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID