产品说明书

Prexasertib

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Chemical Structure| 1234015-52-1 同义名 : Ly2606368;ACR 368
CAS号 : 1234015-52-1
货号 : A853008
分子式 : C18H19N7O2
纯度 : 99%+
分子量 : 365.389
MDL号 : MFCD25977016
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 16 mg/mL(43.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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

2.74mL

0.55mL

0.27mL

13.68mL

2.74mL

1.37mL

27.37mL

5.47mL

2.74mL

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):2004-1

[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.