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编 号:F208717
分子式:C38H46O8
分子量:630.77
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer.

体内研究:
Gambogenic Acid (4-12 mg/kg,静脉注射,每 2 天一次,14 天) 可抑制 SCLC 小鼠异种移植模型中的肿瘤生长。Animal Model:SCLC mouse xenograft model
Dosage:4-12 mg/kg
Administration:i.v., every 2 days, 14 days
Result:Increased the expression of pro-apoptotic proteins (cleaved caspase-3, -8 and -9, Bax, cleaved PARP and p53 proteins).Decreased the anti-apoptotic proteins (Bcl-2).

体外研究:
Gambogenic Acid (0.6-2.4 μM, 1.2-3.2 μM; 24-72 h) 抑制 SCLC 细胞系 (NCI-H446/NCI-H1688) 的增殖。Gambogenic acid (0.6-1.2 μM, 1.5-2.2 μM; 24 h) 将 SCLC 细胞系 (NCI-H446/NCI-H1688) 的细胞周期进程阻滞在不同阶段。Gambogenic acid (1.4-2 μM, 2.4-3 μM; 24 h) 以剂量依赖性方式增加 SCLC 细胞系 (NCI-H446/NCI-H1688) 的细胞凋亡率.
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