货号 | 11602-1mg |
描述 | AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).1,2 It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.1,2 AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.2,3 |
别名 | Barasertib-HQPA; |
供应商 | Cayman |
应用文献 | |
1.Mortlock, A.A.,Foote, K.M.,Heron, N.M., et al. Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J. Med. Chem. 50(9), 2213-2224 (2007). 2.Yang, J.,Ikezoe, T.,Nishioka, C., et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood 110(6), 2034-2040 (2007). 3.Wilkinson, R.W.,Odedra, R.,Heaton, S.P., et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin. Cancer. Res 13(12), 3682-3688 (2007). | |
运输条件 | Wet Ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 507.6 |
分子式 | C26H30FN7O3 |
CAS号 | 722544-51-6 |
稳定性 | ≥ 2 years |
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