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Onvansertib

Catalog No. T6247 CAS 1034616-18-6

Synonyms: NMS-P937, NMS-1286937

Onvansertib (NMS-1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher over PLK2/PLK3.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Onvansertib, CAS 1034616-18-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 239.00
100 mg	In stock	$ 396.00
200 mg	In stock	$ 511.00
500 mg	In stock	$ 829.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.88%

Purity: 99.76%

Purity: 99.41%

Purity: 98.08%

Purity: 97.01%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Onvansertib (NMS-1286937), an oral, specific Polo-like Kinase 1 (PLK1) inhibitor, is with IC50 of 2 nM. The specificity of NMS-P937 forPLK1 is 5000-fold higher over PLK2/PLK3.
Targets&IC50	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. [2]
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]
Kinase Assay	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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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	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)

Synonyms	NMS-P937, NMS-1286937
Molecular Weight	532.52
Formula	C24H27F3N8O3
CAS No.	1034616-18-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 39 mg/mL (73.2 mM)

Ethanol: 10 mg/mL (18.77 mM), Heating is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Beria I, et al. Bioorg Med Chem Lett. 2011, 21(10), 2969-2974. 2. Valsasina B, et al. Mol Cancer Ther. 2012, 11(4), 12006-12016.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Orally Active Compound Library Target-Focused Phenotypic Screening Library Kinase Inhibitor Library Bioactive Compounds Library Max

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Onvansertib 1034616-18-6 Apoptosis Cell Cycle/Checkpoint PLK NMS 1286937 inhibit Inhibitor NMS-P 937 NMS1286937 Polo-like Kinase (PLK) NMS-P-937 NMS-P937 NMS-1286937 inhibitor

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