NMS-1286937
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NMS-1286937 (NMS-P937)是高效选择性的Polo样激酶1(PLK1)抑制剂,IC50值为2 nM [1].
PLK1是一种丝氨酸/苏氨酸蛋白激酶,在细胞周期调控中发挥重要作用.PLK1参与有丝分裂进入\两极有丝分裂纺锤体形成\中心体复制\从中期向后期过渡\维持基因组稳定性和胞质分裂[1].
NMS-1286937是具有口服生物利用度的PLK1抑制剂.从实体瘤\白血病和淋巴瘤建立的细胞系中,NMS-1286937能够抑制肿瘤细胞增殖.在A2780细胞中,NMS-1286937引起细胞周期G2-M期停滞.在有丝分裂期间,NMS-1286937引起染色体错配和异常数量的纺锤体极,从而诱导凋亡性细胞死亡[2].在人骨肉瘤(OS)细胞系中,NMS-1286937抑制细胞迁移和克隆形成能力.在过表达ABCB1\Doxorubicin(DX)耐受的细胞系中,NMS-1286937和DX协同处理能够通过抑制ABCB1转运活性从而还原DX抗性[3].
在Harlan-/-小鼠中,NMS-P937表现出良好的药代动力学特性,具有低清除率,高AUC与Cmax,以及可接受的口服生物利用度.在人HCT116结肠癌细胞异种移植小鼠中,NMS-P937 (45 mg/kg)抑制83%的肿瘤生长,并使体重降低16% [1].
参考文献：
[1]. Beria I, Bossi RT, Brasca MG, 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, 21(10): 2969-2974.
[2]. Valsasina B, Beria I, Alli C, 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, 11(4): 1006-1016.
[3]. Sero V, Tavanti E, Vella S, et al. Targeting polo-like kinase 1 by NMS-P937 in osteosarcoma cell lines inhibits tumor cell growth and partially overcomes drug resistance. Invest New Drugs, 2014, 32(6): 1167-1180.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 532.52 |
| Cas No. | 1034616-18-6 |
| Formula | C24H27F3N8O3 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥13.33 mg/mL in DMSO |
| SDF | Download SDF |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
