ZINC05007751
目录号: PL08451 纯度: ≥98%
ZINC05007751 是一种有效的 NIMA 相关激酶 NEK6 抑制剂,IC50 为 3.4 μM。ZINC05007751 对一组人类癌细胞系显示出抗增殖活性,并且在 BRCA2 突变的卵巢癌细胞系中显示出与顺铂和紫杉醇的协同效应。ZINC05007751 对 NEK1 和 NEK6 具有很强的选择性,但对 NEK2、NEK7 和 NEK9 没有明显的活性。
CAS No. :591239-68-8
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中文名称
ZINC05007751
英文名称
ZINC05007751
英文别名
(5Z)-2-hydroxy-4-methyl-6-oxo-5-[(5-phenylfuran-2-yl)methylidene]-5,6-dihydropyridine-3-carbonitrile;(Z)-4-Methyl-2,6-dioxo-5-((5-phenylfuran-2-yl)methylene)-1,2,5,6-tetrahydropyridine-3-carbonitrile;NEK6 inibitor 8;HMS1370L16;HMS1481J13;STK032295;(5Z)-4-methyl-2,6-dioxo-5-[(5-phenylfuran-2-yl)methylidene]pyridine-3-carbonitrile;ST50265589;(5Z)-4-methyl-2,6-d;ZINC05007751
Cas No.
591239-68-8
分子式
C18H12N2O3
分子量
304.30
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
ZINC05007751 是一种有效的 NIMA 相关激酶 NEK6 抑制剂,IC50 为 3.4 μM。ZINC05007751 对一组人类癌细胞系显示出抗增殖活性,并且在 BRCA2 突变的卵巢癌细胞系中显示出与顺铂和紫杉醇的协同效应。ZINC05007751 对 NEK1 和 NEK6 具有很强的选择性,但对 NEK2、NEK7 和 NEK9 没有明显的活性。
生物活性
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC 50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9.
性状
Solid
体外研究(In Vitro)
ZINC05007751 (6 μM-190 μM; 24 hours) inhibits the growth of MDA-MB-231, PEO1, NCI-H1299 and HCT-15 with IC50 below 100?μM.
ZINC05007751 induces perturbation of PEO1 cell cycle.
ZINC05007751 (ovarian cancer cells PEO1) shows synergism with Cisplatin, resulting in a significant reduction of Cisplatin IC50 from 7.9 to 0.1??μM, with combination ZINC05007751 (44?μM)?+?Cisplatin (10?μM) exhibiting the greatest synergistic effect. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. De Donato M, et al. Identification and antitumor activity of a novel inhibitor of the NIMA-related kinase NEK6. Sci Rep. 2018;8(1):16047. Published 2018 Oct 30.
溶解度数据
In Vitro: DMSO : 8.33 mg/mL (27.37 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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