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  • 產(chǎn)品名稱： NMS-P937
  • 產(chǎn)品貨號(hào)： CS6247
  • 貨期： 現(xiàn)貨
  • 價(jià)格與訂購： 150
  • 數(shù)量：
    庫存： 100
  • 規(guī)格： 2mg 5mg 10mg
  • 產(chǎn)品信息
  • 如何訂購
    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    PLK2    PLK3
    體外活性
    In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. [1]
    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 Supernatant, containing the phosphorylated substrate, is subsequently withdrawn and transferred into a counting plate, followed by evaluation by b-counting.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) Cell lines: 137 solid tumor cell lines, and 43 cell lines derived from leukemias and lymphomasicon
    參考文獻(xiàn)
    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.
    別名
    NMS-1286937 , NMS-1286937
    純度
    99.88%
    分子量
    532.52
    分子式
    C24H27F3N8O3
    CAS No
    1034616-18-6
    存儲(chǔ)
    0-4℃ for short term (days to weeks), or -20℃ for long term (months).
    溶解度
    DMSO: 39 mg/mL (73.2 mM)
    Ethanol: 10 mg/mL (18.77 mM), warmed
    Water: <1 mg/mL
    ( < 1 mg/ml refers to the product slightly soluble or insoluble )
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    Note
    For research use only .