ly-2606368

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

LY2606368 HCl is a selective ATP competitive inhibitor of checkpoint kinase 1 (IC50: 1.5nM in SW1990 cells).

Prexasertib dimesylate (LY2606368 dimesylate) is a highly selective, ATP-competitive, second-generation inhibitor of checkpoint kinase 1 (CHK1), with a K_i of 0.9 nM and an IC_50 of <1 nM, and also effectively inhibits CHK2 (IC_50 = 8 nM) and RSK1 (IC_50 = 9 nM). Its mechanism induces double-stranded DNA breakage and replication catastrophe, leading to apoptosis, and demonstrates potent anti-tumor activity.

Prexasertib is an effective and selective Chk1 Chk2 inhibitor. Prexasertib causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms.

Prexasertib is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 causes replication catastrophe and antitumor effects through CHK1-d