AG 957, Adamantyl Ester is a lipophilic, adamantyl ester form of tyrphostin AG 957 that displays anti-proliferative properties. The product has been shown to be selective and is ~3-4 fold more potent than the bcr/abl kinase inhibitor AG 957. AG 957, Adamantyl Ester Downregulates p210bcr/abl autokinase activity (IC50 = 14 µM). Selectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC50 = 9.8 µM) by inducing apoptosis. AG 957, Adamantyl Ester is reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC50 ~0.1-0.25 µM).
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