Onvansertib NEW
Price | $30 | $64 | $89 |
Package | 1mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: Onvansertib | CAS No.: 1034616-18-6 |
Purity: 99.88% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | Onvansertib |
Description | Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth. |
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) |
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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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. |
In vitro | METHODS: 137 tumor cells were treated with Onvansertib for 72 h. Cell viability was measured by CellTiter-Glo Assay. RESULTS: Sixty of the 137 cell lines had IC50 values below 100 nmol/L, and only 9 cell lines had IC50 values above 1 μmol/L, indicating a wide range of activity. [1] METHODS: Cisplatin-sensitive and -resistant CAL33 were treated with Onvansertib (25-50 nM) for 24 days, and the cell cycle was examined by Flow cytometry. RESULTS: Onvansertib treatment induced accumulation of all sensitive and resistant CAL33 cells in G2/M phase in a dose-dependent manner. [2] |
In vivo | METHODS: To test the antitumor activity in vivo, Onvansertib (60 mg/kg) was administered orally to Hsd, athymic nu/nu mice bearing HCT116 xenografts once daily for eight days. RESULTS: Onvansertib was able to achieve good antitumor activity with minimal weight loss and inhibited tumor growth to a considerable extent with a TGI of 79%. [1] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 55 mg/mL (103.28 mM) Ethanol : 10 mg/mL (18.77 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
Keywords | NMS 1286937 | inhibit | Inhibitor | Apoptosis | NMS-P 937 | NMS1286937 | Onvansertib | Polo-like Kinase (PLK) | NMS-P-937 |
Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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