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