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AZ960

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Chemical Structure| 905586-69-8 同义名 : -
CAS号 : 905586-69-8
货号 : A147841
分子式 : C18H16F2N6
纯度 : 97%
分子量 : 354.357
MDL号 : MFCD16621127
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(84.66 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JAK2

    JAK2, Ki:0.45 nM

    JAK2, IC50:<3 nM
描述 The Janus-associated kinase (Jak) family, comprised 4 different protein-tyrosine kinases, Jak1, Jak2, Jak3, and TYK2, plays an important role in cellular survival, proliferation, and differentiation. Jak kinases are key mediators of signaling downstream of a variety of cytokine and/or growth factor receptors. Each Jak possesses kinase domain, a catalytically inactive pseudokinase, and amini-terminal, ezrin, radixin, and moesin (FERM). Cytokine receptors bind to FERM domain, leading to activation of Jaks, which create docking sites for members of signal transducers and activators of transcription (Stat) family, including Stat3 and Stat5. AZ960 is a potent and selective ATP competitive inhibitor of the Jak2 kinase with a Ki of 0.45 nM. AZ960 was also shown to be active against other kinases, including TrkA, Aurora-A, and FAK, with IC50 of around 0.1 μM. In a vitro study, HTLV-1 (human T-cell lymphotropic virus type 1) - infected T cells cells were incubated with AZ960 (0.3 or 1 μM) for 2 days and the result showed that AZ960 suppressed the growth of MT-1 and MT-2 cells with IC50 of 0.8 and 1 μM. Intact GV-oocytes were cultured with CEP-33779 for 12 h to inhibit JAK2 activity during maturation. The result showed that a large proportion of the CEP-33779 treated oocytes failed to extrude polar body I, only 21.14 ± 4.03% (n=382) of these oocytes reached the M II stage after 12 h in vitro maturation, a rate significantly lower than that of non-treated control oocytes (81.44±3.64%, n=357)[3]. HTLV-1-infected T cells and MOLT-4 cells (5 × 105 cells/mL) were cultured with various concentrations of AZ960 (0.03-1 μM) for 2 days. AZ960 inhibited the growth of freshly isolated ATL (Adult T-cell leukemia/lymphoma) cells in a dose-dependent manner with IC50 of 0.3 μM, and AZ960 also inhibited the growth of MOLT-4 cells in a dose-dependent manner with IC50 of 1.2 μM, which indicated blockade of Jak2/Stats by Jak2 kinase inhibitor AZ960 represents a promising treatment strategy for individuals with ATL.
作用机制 AZ 960 binds to the ATP-binding site of JAK2 kinase.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.82mL

0.56mL

0.28mL

14.11mL

2.82mL

1.41mL

28.22mL

5.64mL

2.82mL
参考文献

[1]Yang J, Ikezoe T, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95.

[2]Gozgit JM, Bebernitz G, 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 Nov 21;283(47):32334-43.

[3]Yang J, Ikezoe T, Nishioka C, Furihata M, Yokoyama A. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95. doi: 10.1158/1535-7163.MCT-10-0416. PMID: 21159615.