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Onvansertib (NMS-P937)

Name: Onvansertib (NMS-P937)
Brand: Selleck Chemicals
SKU: S7255
Rating: 5 (4 reviews)

Catalog No.S7255 Synonyms: PCM-075, NMS1286937

For research use only.

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.

Onvansertib (NMS-P937) Chemical Structure

CAS No. 1034616-18-6

Selleck's Onvansertib (NMS-P937) has been cited by 4 Publications

Purity & Quality Control

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PLK Signaling Pathway Map

Biological Activity

Description

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	NFrtdnhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=				NUPPZYNMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{whUUN3MDC9JFAvODR{IN88UU4>	NHLhO\|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS3NFg3Oid-MkG0O\|A5PjJ:L3G+
CAL51	MVfD[YxtKGO7Y3zlJIF{e2G7	NFW1Om8xNjFidH:gNUB2VQ>?	M{\SSVI1KGi{cx?=		MXLD[YxtKGO7Y3zlJIFzemW\|dDDpckBpfW2jbjDDRWw2OSClZXzsd{BifCByLkGgeI8hOSC3TTDh[pRmeiB{NDDodpMh[nliZnzve{BkgXSxbXX0dpk>	NGXQfZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS3NFg3Oid-MkG0O\|A5PjJ:L3G+

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 (from reference)

Kinase Assay:^[1]

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]

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.

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	532.52
Formula	C₂₄H₂₇F₃N₈O₃
CAS No.	1034616-18-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1CCN(CC1)C2=CC(=C(C=C2)OC(F)(F)F)NC3=NC=C4CCC5=C(C4=N3)N(N=C5C(=O)N)CCO

Download Onvansertib (NMS-P937) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03829410	Recruiting	Drug: Onvansertib\|Biological: Bevacizumab\|Drug: FOLFIRI	Metastatic Colorectal Cancer\|KRAS Gene Mutation	Cardiff Oncology	May 6 2019	Phase 1\|Phase 2
NCT03303339	Completed	Drug: Onvansertib\|Drug: Cytarabine\|Drug: Decitabine	Acute Myeloid Leukemia	Cardiff Oncology	November 17 2017	Phase 1\|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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