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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Polo-like Kinase (PLK)-NMS-P937
NMS-P937

Chemical Structure : NMS-P937

CAS No.: 1034616-18-6

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NMS-P937 (Onvansertib, NMS-1286937)

货号: PC-22312Not For Human Use, Lab Use Only.

NMS-P937 (Onvansertib, NMS-1286937) is a potent, selective and orally available PLK1 inhibitor with IC50 of 2 nM.

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10 mg ￥1180 In stock
50 mg ￥2480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NMS-P937 (Onvansertib, NMS-1286937) is a potent, selective and orally available PLK1 inhibitor with IC50 of 2 nM, >300-fold selective over PLK2/3.
NMS-P937 exhibits antiproliferative effect on A2780 cells with IC50 of 42 nM.
NMS-P937 potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits xenograft tumor growth with clear PLK1-related mechanism of action at well-tolerated doses in mice after oral administration.
NMS-P937 shows potential for combination in clinical settings with approved cytotoxic drugs, causing tumor regression in HT29 human colon adenocarcinoma xenografts upon combination with irinotecan and prolonged survival of animals in a disseminated model of acute myelogenous leukemia in combination with cytarabine.

物理化学性质&存储条件

分子量 532.53
分子式 C24H27F3N8O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(2-Hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

参考文献

1. Beria I, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74.

2. Valsasina B, et al. Mol Cancer Ther. 2012 Apr;11(4):1006-16.

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