产品
编 号:F752139
分子式:C54H63FN5O10P
分子量:992.08
产品类型
结构图
CAS No: 2408917-12-2
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产品详情
生物活性:
Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways.
体内研究:
Antitumor agent-61 (compound 6b) (10-20 mg/kg; i.h.; Twice daily, for 28 days; BALB/c nude mice with SK-OV-3 xenograft) reduces mean NPC tumor burden in a dose-dependent manner.Animal Model:BALB/c nude mice with SK-OV-3 xenograft
Dosage:10 and 20 mg/kg
Administration:Subcutaneous injection; Twice daily, for 28 days.
Result:Suppressed tumor growth by 47.7% and 56.8% for 10 and 20 mg/kg, respectively, without affecting body weight or causing any overt adverse effects.
体外研究:
Antitumor agent-61 (compound 6b) shows anti-proliferation activity with IC50 values of 3.05, 2.20, 3.23, 1.75, 0.92 and 1.39 μM for A549, MCF-7, MG-63, U2OS, SK-OV-3 and SK-OV-3/CDDP cells.Antitumor agent-61 (compound 6b) (50-150 μM) shows a certain inhibitory activity against Topo I at 150 μM.Antitumor agent-61 (compound 6b) (5-10 μM; 24 hours, SK-OV-3 cells) induces apoptosis through mitochondrial pathway. Decrease the MMP level and increase ROS level in a dose-dependent manner .