AZD-1480产品描述：AZD-1480 是一种新颖的 JAK2 的ATP竞争性抑制剂，IC₅₀ 值为 < 0.4 nM。
AZD-1480产品描述：AZD-1480 is a novel ATP-competitive JAK2 inhibitor with IC₅₀ of < 0.4 nM, selectively against JAK3 ａnd Tyk2, ａnd to a smaller extent against JAK1.IC50 & Target: IC50: < 0.4 nM (JAK2)In Vitro: AZD1480 (5μM) induces G2/M arrest ａnd cell death by inhibiting Aurora kinases^[1]. AZD1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 ａnd STAT3 signaling ａnd downstream targets including Cyclin D2 in human multiple myeloma cells. At low micromolar concentrations, AZD1480 blocks cell proliferation ａnd induces apoptosis of myeloma cell lines^[2]. AZD1480 effectively blocks constitutive ａnd stimulus-induced JAK1, JAK2, ａnd STAT-3 phosphorylation in both human ａnd murine glioma cells, ａnd leads to a decrease in cell proliferation ａnd induction of apoptosis^[3]. AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, ａnd that it is capable of inhibiting STAT3 phosphorylation ａnd tumor growth in a STAT3-dependent manner. AZD1480 inhibits tumor angiogenesis ａnd metastasis in part by affecting the tumor microenvironment^[4].In Vivo: AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors ａnd multiple myeloma^[1]. In vivo, AZD1480 inhibits the growth of subcutaneous tumors ａnd increases survival of mice bearing intracranial glioblastoma (GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480 should be considered for study in the treatment of patients with GBM tumors^[3]. AZD1480 blocks lung infiltration of myeloid cells ａnd formation of pulmonary metastases in both mouse syngeneic experimental ａnd spontaneous metastatic models. Furthermore, AZD1480 reduces angiogenesis ａnd metastasis in a human xenograft tumor model^[4]. AZD1480 suppresses the growth of human solid tumor xenografts harboring persistent Stat3 activity^[5].

研究领域：GPCR/G Protein

靶点：Adrenergic Receptor

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Alternative_Names:AZD1480;AZD 1480

MWt:348.77

Formula:C14H14ClFN8

SMILES:ClC1=C(N=C(N=C1)N[C@@H](C)C2=NC=C(C=N2)F)NC3=NNC(C)=C3

Research_Area:Cancer



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