Onvansertib
作者：齊岳
發(fā)布時(shí)間：2023-09-05
08:51:42
點(diǎn)擊數(shù)：
產(chǎn)品名稱(chēng)：Onvansertib
產(chǎn)品描述：
| 產(chǎn)品描述 | NMS-P937 (NMS1286937), 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. |
| 靶點(diǎn)活性 | PLK1:2 nM |
| 體外活性 | 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] |
| 體內(nèi)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] |
| 激酶實(shí)驗(yàn) | 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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 別名 | NMS-P937, NMS-1286937 |
| 分子量 | 532.52 |
| 分子式 | C24H27F3N8O3 |
| CAS No. | 1034616-18-6 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 39 mg/mL (73.2 mM)
Ethanol: 10 mg/mL (18.77 mM),warmed
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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