GZD824 - CAS# 1257628-77-5 ne Protease inhibitor Hydrochloride RN-1 exhibits good brain penetration

RN-1 exhibits good brain penetration and retention

cell-permeable

108(1291):1252-6

26-tetramethyl-4-oxo-22-[3-oxo-3-[(E

giving growth delays in A431 xenografts exceeding 50 days following oral administration

GZD824 - CAS# 1257628-77-5 ne Protease inhibitor Hydrochloride RN-1 exhibits good brain penetrationOlverembatinib, also known as GZD824, is a novel orally bioavailable inhibitor against a broad spectrum of Bcr Abl mutants including T315I. 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,