gzd824-dimesylate

Description: GZD824 Dimesylate, the dimesylate salt of GZD-824 (HQP1351; HQP-1351), is a novel, potent orally bioavailable Bcr-Abl inhibitor with potential antineoplastic activity. It inhibits Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 tightly bound to Bcr-Abl(WT) and Bcr-Abl(T315I) with K(d) values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase functions with nanomolar IC(50) values. GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. GZD824 represents a promising and new lead candidate for development of Bcr-Abl inhibitors to overcome acquired imatinib resistance.

References: J Med Chem. 2013 Feb 14; 56(3):879-94.

Related CAS: 1257628-77-5 (free base)