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XL228是多靶点的酪氨酸激酶抑制剂,对Bcr-Abl,Aurora A,IGF-1R,Src 和 Lyn 的IC50 值分别为5,3.1,1.6,6.1,2 nM。
中文名称:
N4-(5-环丙基-1H-吡唑-3-基)-N2-[[3-异丙基-5-异恶唑基]甲基]-6-(4-甲基-1-哌嗪基)-2,4-嘧啶二胺
[1]. Cortes J, et al. Preliminary Clinical Activity in a Phase I Trial of the BCR-ABL/IGF- 1R/Aurora Kinase Inhibitor XL228 in Patients with Ph++ Leukemias with Either Failure to Multiple TKI Therapies or with T315I Mutation. Blood 2008 112:3232
[2]. Douglas O, et al. Abstract C192: Characterization of the target profile of XL228, a multi‐targeted protein kinase inhibitor in phase 1 clinical development. Mol Cancer Ther 2009;8(12 Suppl):C192.
[3]. Shah N, et al. Targeting Drug-Resistant CML and Ph+-ALL with the Spectrum Selective Protein Kinase Inhibitor XL228. Blood 2007 110:474;
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