| 货号 | 16298-25mg |
| 描述 | Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).1 Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.2 XL019 is a potent, bioavailable JAK inhibitor with preference for JAK2 (IC50 = 2 nM) over JAK1 and JAK3 (IC50s = 130 and 250 nM, respectively).3,4 It is effective against JAK2V617F as well as JAK2 and inhibits phosphorylation of STAT5 in vivo.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gozgit, J.M.,Bebernitz, G.,Patil, P., et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. The Journal of Biological Chemisty 283(47), 32334-32343 (2008). 2.Yang, J.,Ikezoe, T.,Nishioka, C., et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Molecular Cancer Therapeutics 9(12), 3386-3395 (2010). 3.Forsyth, T.,Kearney, P.C.,Kim, B.G., et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorganic & Medicinal Chemistry Letters 22(24), 7653-7658 (2012). 4.Verstovsek, S. Therapeutic potential of JAK2 inhibitors. Hematology Am.Soc.Hematol.Educ.Program 2009(1), 636-642 (2009). 5.Furqan, M.,Mukhi, N.,Lee, B., et al. Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical application. Biomark.Res. 1(1), 1-10 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥90% |
| 计算分子量 | 444.5 |
| 分子式 | C25H28N6O2 |
| CAS号 | 945755-56-6 |
| 稳定性 | ≥ 2 years |
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