Molecular Formula | C14H14ClFN8 |
Molar Mass | 348.77 |
Density | 1.517 |
Melting Point | >205°C (dec.) |
Boling Point | 575.2±60.0 °C(Predicted) |
Solubility | Chloroform (Slightly, Heated), DMSO (Slightly, Heated), Methanol (Slightly, Heat |
Appearance | powder |
Color | white to beige |
pKa | 13.73±0.10(Predicted) |
Storage Condition | -20°C |
In vitro study | 5 M AZD1480 induced cell cycle stop in G2/M phase, and induced cell death by inhibiting Aurora kinase. AZD1480 is a potent inhibitor of JAK2, acting on human multiple myeloma cells, inhibiting growth, survival, FGFR3 and STAT3 signaling, and downstream targets including Cyclin D2. At low micromolar concentrations, AZD1480 inhibits cell proliferation and induces apoptosis in myeloma cell lines. AZD1480 acts on human and murine glioma cells and effectively inhibits the phosphorylation of constitutive and inducible JAK1, JAK2, and STAT-3, resulting in decreased cell proliferation and induction of apoptosis. AZD1480 is a potent ATP-competitive small molecule inhibitor of JAK1/2 kinase that inhibits STAT3 phosphorylation and tumor growth in a stat3-dependent manner. AZD1480 inhibits tumor angiogenesis and local metastasis by affecting the tumor microenvironment. |
In vivo study | AZD1480 inhibits STAT3 phosphorylation in human solid tumor models and multiple myeloma models. In Vivo, AZD1480 inhibits the growth of subcutaneous xenografts and increases the lifespan of mice carrying intracranial malignant glioma (GBM) by Inhibiting STAT3 activity, this indicates that the pharmacology of AZD1480 inhibition of the JAK/STAT3 pathway can be used to study the treatment of patients with intracranial malignant glioma. AZD1480 inhibits lung infiltration of bone marrow cells and lung metastases. AZD1480 reduces angiogenesis and metabolism in human xenograft models. AZD1480 inhibits the growth of human solid tumors containing STAT activity. |
HS Code | 29335990 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.867 ml | 14.336 ml | 28.672 ml |
5 mM | 0.573 ml | 2.867 ml | 5.734 ml |
10 mM | 0.287 ml | 1.434 ml | 2.867 ml |
5 mM | 0.057 ml | 0.287 ml | 0.573 ml |
biological activity | AZD1480 is a novel, ATP-competitive JAK2 inhibitor with an IC50 of 0.26 nM, selective effect on JAK3 and Tyk2, the effect on JAK1 is weak. Phase 1. AZD1480 is a novel, ATP-competitive JAK2 inhibitor with an IC50 of 0.26 nM in a cell-free assay. It acts selectively on JAK3 and Tyk2 and has a weak effect on JAK1. Phase 1. |
characteristics | AZD1480 is a potential novel therapeutic agent for the treatment of multiple myeloma. |
Target | Value |
JAK2 (Cell-free assay) | 0.26 nM |