ZINC05007751

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ZINC05007751

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CAS NO:

591239-68-8

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 kinaseNEK6inhibitor with anIC₅₀of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of humancancercell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovariancancercell 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].

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

性状

Solid

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℃)

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。