化合物NMS-P937 T6247

Product Introduction
Bioactivity


英文名: Onvansertib

描述: Onvansertib (NMS-1286937) 是一种可口服的高选择性PLK1抑制剂，IC50值为 2 nM。

细胞实验: 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)

激酶实验: 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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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.

体外活性: 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]

体内活性: 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]

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

溶解度: DMSO : 39 mg/mL (73.2 mM)
Ethanol : 10 mg/mL (18.77 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: NMS 1286937 | inhibit | Inhibitor | Apoptosis | NMS-P 937 | NMS1286937 | Onvansertib | Polo-like Kinase (PLK) | NMS-P-937

相关产品: Alpha-Hederin | BML-277 | Hesperetin | Quizartinib | K-Ras(G12C) inhibitor 12 | Meclizine dihydrochloride | OSI-930 | Linderalactone | CM-272 | Capsazepine

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Preclinical Compound Library

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