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编 号:F756782
分子式:C32H33ClN6O3S
分子量:617.16
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生物活性:
LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis.

体内研究:
LSD1-IN-25 (Compound 9j; 10 and 20 mg/kg; oral; once daily for 21 days) 在 H1650 细胞的小鼠异种移植模型中显示出抗肿瘤活性。Animal Model:Nude mice, xenograft model of H1650 cells
Dosage:10 mg/kg and 20 mg/kg
Administration:Oral, once daily for 21 days
Result:Presented a remarkable reduction of average tumor weight by 41.5% and 64.0% at dosages of 10 and 20 mg/kg, respectively. Evidently prolonged the mice's survival.

体外研究:
LSD1-IN-25 (Compound 9j; 0-20 μM; 72 h) 抑制实体瘤细胞增殖。LSD1-IN-25 (1-4 μM; 24 h) 诱导细胞 H3K4me2 升高,抑制 H1650 细胞的 EMT 过程。LSD1-IN-25 (1-4 μM; 24 h) 诱导 H1650 细胞凋亡和 S 阻滞。
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