| 货号 | 10702-1mg |
| 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 AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).2,3 It is selective for JAK2 over other JAK family members as well as a panel of related kinases.3 AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).3 It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.3 AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.2,3 In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.4,5 |
| 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.Hedvat, M.,Huszar, D.,Herrmann, A., et al. The JAK2 inhibitor AZD1480 potently blocks stat3 signaling and oncogenesis in solid tumors. Cancer Cell 16, 487-497 (2009). 3.Ioannidis, S.,Lamb, M.L.,Wang, T., et al. Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. Journal of Medicinal Chemistry 54(1), 262-276 (2010). 4.Scuto, A.,Krejci, P.,Popplewell, L., et al. The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival. Leukemia 25(3), 538-550 (2011). 5.Xin, H.,Herrmann, A.,Reckamp, K., et al. Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480. Cancer Research 71(21), 6601-6610 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 348.8 |
| 分子式 | C14H14ClFN8 |
| CAS号 | 935666-88-9 |
| 稳定性 | ≥ 2 years |
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