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CAS No. : 477-47-4
MCE 国际站:Picropodophyllin
产品活性:Picropodophyllin (AXL1717) 是选择性的胰岛素样生长因子-1受体 (IGF-1R)抑制剂,IC50 为1 nM。
研究领域:Protein Tyrosine Kinase/RTK | Apoptosis
In Vitro: Picropodophyllin (AXL1717) (0.5, 2.5, 10 μM) potently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation in intact cells. Picropodophyllin (AXL1717) also inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells. Picropodophyllin (AXL1717) synergistically sensitizes HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199 via further decreasing cell viability and enhancing apoptosis. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells.
In Vivo: Picropodophyllin (AXL1717) (20 mg/kg/12 h, i.p.) causes complete tumor regression in SCID mice xenografted with human ES-1, BE, and PC3. Picropodophyllin (AXL1717) shows a potent antitumor activity, increases survival in the 5T33MM mouse model.
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