(E,E)-2-(Benzylaminocarbonyl)-3-(3,4-dihydroxystyryl)acrylonitrile Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable hydroxystryrylacrylonitrile tyrosine kinase inhibitor that displays anti-tumor properties. Potently inhibits the kinase activities of JAK2 and Bcr-Abl (IC50 ~100-600 nM and 500-700 nM, respectively), and displays excellent selectivity over other tyrosine kinases, Btk, Lck, Lyn, Src, Syk and ZAP-70 (IC50 > 5 µM). 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. Reported to be much more potent than AG 490 (Cat. No. 658401) in inducing ALL cells growth arrest (IC50 ~ 120 nM vs. 5-25 µM). Its in vivo efficacy in cancer reduction has been successfully demonstrated in NOD-SCID mice engrafted with human Ph+ ALL cells. Purity: ≥95% by HPLC. Ref.: Demin, P., et al. 2004. Bioorg. Med. Chem. 12, 3019. Grunberger, T., et al. 2003. Blood 102, 4153. |
