产品描述: | 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 |
靶点: |
MAPK |
体外研究: |
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. Cell Cytotoxicity Assay 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. |
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. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.286 ml |
16.431 ml |
32.862 ml |
5 mM |
0.657 ml |
3.286 ml |
6.572 ml |
10 mM |
0.329 ml |
1.643 ml |
3.286 ml |
50 mM |
0.066 ml |
0.329 ml |
0.657 ml |
|
注意: |
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