Tyrene CR4 is a cell-permeable, reversible, and substrate competitive hydroxystryrylacrylonitrile tyrosine kinase inhibitor that show anti-tumor properties. Tyrene CR4 potently inhibits JAK2 and Bcr-Abl (the fusion protein of Bcr and c-Abl) (IC50 ~100-600 nM and 500-700 nM, respectively) by targeting their kinase activities. Tyrene CR4 displays excellent selectivity over other tyrosine kinases, Btk, Lck, Lyn, Src, Syk and ZAP-70 (IC50 >5 μM). Tyrene CR4 has been shown to preferentially induce apoptosis in acute lymphoblastic (ALL) and myeloid leukemia cells (AML), while exhibiting little deleterious effect towards normal bone marrow cell differentiation and proliferation. Tyrene CR4 has also been reported to be more potent than AG 490 (sc-202046) in inducing ALL cells growth arrest (IC50 ~ 120 nM vs. 5-25 μM).
Demin, P., et al. 2004. Bioorg. Med. Chem. 12, 3019. Grunberger, T., et al. 2003. Blood 102, 4153.
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