LY2606368 dihydrochloride

• CAT Number: I000927
• CAS Number: 1234015-54-3
• Molecular Formula: C18H21Cl2N7O2
• Molecular Weight: 438.31
• Purity: ≥95%
• Target: Chk1
• Solubility: DMSO: ≥ 32 mg/mL
• Storage: Store at -20C
• IC50: 1.5 nM (SW1990 cell line) [1]

Cell cycle checkpoint kinase 1 (ChK1) plays a crucial role in the DNA damage response (DDR) and is a serine/threonine protein kinase. Prexasertib (LY2606368) is an ATP-competitive inhibitor that specifically targets CHK1 with a Ki value of 0.9 nM. In cell-free experiments, LY2606368 exhibits IC50 values of 8 nM and 9 nM for CHK2 and RSK, respectively. This potent inhibitor holds promise for therapeutic interventions aimed at targeting ChK1 and related signaling pathways involved in the DDR.

Reference

[1]. Wenjuan Wu, et al. Abstract 1776: Antitumor activity of Chk1 inhibitor LY2606368 as a single agent in SW1990 human pancreas orthotopic tumor model. Cancer Res April 15, 2012; 72(8 Supplement): 1776