ZINC05007751

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ZINC05007751  纯度: 98.47%

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。

ZINC05007751

ZINC05007751 Chemical Structure

CAS No. : 591239-68-8

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50 mg ¥9500 In-stock
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ZINC05007751 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library

生物活性

ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 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[1].

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[1].
ZINC05007751 induces perturbation of PEO1 cell cycle[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231, PEO1, NCI-H1299 and HCT-15 cells
Concentration: 6 μM-190 μM
Incubation Time: 24 hours
Result: Inhibited the growth of MDA-MB-231, PEO1, NCI-H1299 and HCT-15.

分子量

304.30

Formula

C18H12N2O3

CAS 号

591239-68-8

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)

溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (27.37 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2862 mL 16.4312 mL 32.8623 mL
5 mM 0.6572 mL 3.2862 mL 6.5725 mL
10 mM 0.3286 mL 1.6431 mL 3.2862 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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.

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