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Chemical Structure| 1034616-18-6 同义名 : NMS-P937;Nms-1286937;PCM-075
CAS号 : 1034616-18-6
货号 : A443707
分子式 : C24H27F3N8O3
纯度 : 99%+
分子量 : 532.518
MDL号 : MFCD26793840
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(37.56 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PLK1

    PLK1, IC50:2 nM
描述 NMS-1286937 is a potent, selective, and orally available inhibitor of Polo-like kinase 1 (PLK1), boasting an IC50 of 2 nM. This compound also exhibits inhibitory effects on FLT3, MELK, and CK2 with IC50 values of 510, 744, and 826 nM, respectively[1]. NMS-P937 possesses a pure ATP competitive mechanism with a reversible dissociation and no time dependency. At a concentration of 10 μM, NMS-P937 (another name for NMS-1286937) demonstrates selectivity with only marginal activity, inhibiting PLK2 and PLK3 by 48% and 40%, respectively. It displays antiproliferative effects against a wide array of cell lines, achieving IC50 values below 100 nM in 60 out of 137 tested cell lines, with only 9 cell lines exhibiting IC50 values higher than 1 μM[2]. NMS-P937 shows notable cytotoxic activity against AmL-NS8 cells with an IC50 of 36 nM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.39mL

1.88mL

0.94mL

18.78mL

3.76mL

1.88mL
参考文献

[1]Beria I, et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74.

[2]Valsasina B, et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther. 2012 Apr;11(4):1006-16.

[3]Casolaro A, et al. The Polo-Like Kinase 1 (PLK1) inhibitor NMS-P937 is effective in a new model of disseminated primary CD56+ acute monoblastic leukaemia. PLoS One. 2013;8(3):e58424.