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Onvansertib (NMS-1286937, NMS-P937) PLK1 inhibitor

Name: Onvansertib (NMS-1286937, NMS-P937)
Brand: Selleck Chemicals
SKU: S7255
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S7255

Onvansertib (NMS-1286937, NMS-P937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. This compound potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.

Chemical Structure

Molecular Weight: 532.52

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
A2780	Antiproliferative assay			Antiproliferative activity against human A2780 cells, IC50 = 0.042 μM.	21470862
CAL51	Cell cycle assay	0.1 to 1 uM	24 hrs	Cell cycle arrest in human CAL51 cells at 0.1 to 1 uM after 24 hrs by flow cytometry	21470862
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	532.52	Formula	C₂₄H₂₇F₃N₈O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1034616-18-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (93.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.35mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PLK1 ^[1] 2 nM
In vitro	Onvansertib (NMS-1286937, NMS-P937) shows a broad-spectrum antiproliferative activity against different solid tumor, leukemias and lymphomas cell lines. It potently causes a mitotic cell-cycle arrest followed by apoptosis in A2780 cells. ^[2]
Kinase Assay	Kinase profile
Kinase Assay	Onvansertib (NMS-1286937, NMS-P937) inhibitory activity 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.
In vivo	Onvansertib (NMS-1286937, NMS-P937) shows significant tumor growth inhibition in mice xenografted with human HCT116 colon adenocarcinoma cells at 90 mg/kg/d i.v. or p.o. ^[1] In mice bearing HT29, Colo205 colorectal, or A2780 ovarian xenograft tumors, it inhibits xenograft tumor growth. In addition, this compound, in combination with approved cytotoxic drugs, causes enhanced tumor regression and prolongs survival of animals. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/21470862/ [2] https://pubmed.ncbi.nlm.nih.gov/22319201/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05593328	Active not recruiting	Colorectal Cancer\|Metastatic Colorectal Cancer	Cardiff Oncology	March 17 2023	Phase 2
NCT03829410	Completed	Metastatic Colorectal Cancer\|KRAS Gene Mutation	Cardiff Oncology	May 6 2019	Phase 1\|Phase 2
NCT03303339	Completed	Acute Myeloid Leukemia	Cardiff Oncology	November 17 2017	Phase 1\|Phase 2

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