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G5-7

CAS No. : 939681-36-4

MCE 国际站：G5-7

产品活性：G5-7 是具有口服活性的 JAK2 变构抑制剂，可通过结合到 JAK2，选择性的抑制 JAK2 介导的 EGFR 和 STAT3 的磷酸化和激活。G5-7 诱导细胞周阻滞和诱导凋亡、具有抗血管生成活性。G5-7 有用于胶质瘤研究的潜能。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis

作用靶点：JAK  |  Apoptosis

In Vitro: G5-7 (0-5 μM) inhibits EGFR tyrosine phosphorylation and downstream mTOR signaling and arrests the cell cycle at G2 phase.
G5-7 does not directly inhibit EGFR activation.
G5-7 (0-10 μM) comparably increases the abundance of markers (cleved-PARP and caspase 3) of apoptosis in parental LN229 cells and U87MG/EGFRvIII cells.
G5-7 interacts with full-length JAK2.
G5-7 significantly inhibits EGFR Tyr1068 phosphorylation but had no effect on EGFR Tyr1045 phosphorylation.
G5-7 downregulates the downstream signaling of JAK by mTOR.

In Vivo: G5-7 (10 and 50 mg/kg, oral gavege) decreases VEGF secretion and exerts a potent antiangiogenic effect.

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