Tyrene CR4用途
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Tyrene CR4是一种具有抗肿瘤特性的细胞渗透性，可逆性和底物竞争性羟基苯乙烯基丙烯腈酪氨酸激酶抑制剂。酪氨酸CR4通过靶向其激酶活性，有效抑制JAK2和Bcr-Abl（Bcr和c-Abl的融合蛋白）（分别为IC | 50 |〜100-600 nM和500-700 nM）。与其他酪氨酸激酶Btk，Lck，Lyn，Src，Syk和ZAP-70相比，Tyrene CR4表现出优异的选择性（IC | 50 |> 5μM）。业已表明，Tyrene CR4可优先诱导急性淋巴细胞（ALL）和髓样白血病细胞（AML 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) (IC|50|~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 (IC|50|>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 in inducing ALL cells growth arrest (IC|50|~ 120 nM vs. 5-25 μM).
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