同义名 :	LY2606368 Mesylate Hydrate; LY2940930
	CAS号 :	1234015-57-6
	货号 :	A1177301
	分子式 :	C19H25N7O6S
	纯度 :	99%+
	分子量 :	479.51
	MDL号 :	N/A
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-

生物活性

描述

Prexasertib (LY2606368) is distinguished as a highly selective and ATP-competitive second-generation inhibitor of checkpoint kinase 1 (CHK1), possessing a Ki value of 0.9 nM and an IC50 of less than 1 nM. Its ability to inhibit CHK1 with such potency underlines its mechanism of action, which involves causing double-stranded DNA breaks and replication catastrophe, leading to apoptosis. Beyond CHK1, Prexasertib exhibits inhibition against CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM), demonstrating its broad spectrum of action against other kinases involved in cell cycle regulation and tumor growth[1].[2].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.09mL 0.42mL 0.21mL	10.43mL 2.09mL 1.04mL	20.85mL 4.17mL 2.09mL

参考文献
[1]King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13. [2]Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483.