应用 |
An inhibitor of JAK2 |
产品介绍 |
AZD1480是ATP竞争性JAK2抑制剂,IC50为0.26 nM,对JAK1抑制性较弱。 |
备注 |
AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1/2. |
生化机理 |
AZD1480 demonstrated significant immunoregulatory effects by downregulating T-helper 2 cytokines and chemokines, including IL-13 and thymus- and activation-regulated chemokine, and the surface expression of the immunosuppressive programmed death ligands 1 and 2. Higher concentrations of AZD1480 (5μ) induced G2/M arrest and cell death by inhibiting Aurora kinases |
别名 |
AZD1480;AZD 1480; 5-氯-N2-((1S)-1-(5-氟-2-嘧啶基)乙基)-N4-(5-甲基-1H-吡唑-3-基)-2,4-嘧啶二胺;;AZD1480;AZD 1480;5-chloro-n2-((1s)-1-(5-fluoro-2-pyrimidinyl)ethyl)-n4-(5-methyl-1h-pyrazol-3-yl)-2,4-pyrimidinediamine;(S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine |