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编 号:F748948
分子式:C19H15N3O2
分子量:317.34
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生物活性:
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models.

体内研究:
Anticancer agent 109 (3 mg/kg,腹腔注射,A549 肿瘤模型 3 1天,PANC-1 肿瘤模型 85 天,每周 6 次) 在裸鼠异种移植模型中显著降低肿瘤的大小和重量。Animal Model:A549 or PANC-1 xenografted in BALB/c-nu mice.
Dosage:1 mg/kg; 3 mg/kg
Administration:Intraperitoneal injection (i.p.) 6 times a week
Result:Promoted tumor regression to around a quarter with 1 mg/kg, smaller but not eliminated with 3 mg/kg in A549 models.Promoted tumor regression to around a quarter with 3 mg/kg in PANC-1 models.

体外研究:
Anticancer agent 109 (10 μM,48 小时) 抑制 A549 细胞 Gas6 和 Axl,抑制 PANC-1 细胞 Gas6-Axl 轴相关蛋白,诱导 G1 期阻滞并促进晚期凋亡,但不改变 DNA 合成。
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