AZ 960 (AZ960)是一种新型的ATP竞争性的JAK2抑制剂,Ki值为0.45 nM,IC50 < 3 nM,但对于其它JAK家族成员抑制作用较小。对于白血病,AZ960具有一定的抗癌效果,它能显著抑制AML细胞的克隆性生长,并诱导细胞凋亡。
参考文献
1.Yang J, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010;9(12):3386-3395.
2.Ikezoe T, et al. Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia. Int J Cancer. 2011;129(10):2512-21.
3.Valenciano AL, et al. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. Bioorg Med Chem. 2016;24(19):4647-51.
4.Gozgit JM, et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008;283(47):32334-43.
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