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编 号:F232149
分子式:C19H23N3O4
分子量:357.4
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生物活性:
CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research.

体内研究:
CPUY201112 (5-40 mg/kg, i.p., daily, 3 weeks) 在 MCF-7 肿瘤异种移植模型中抑制了肿瘤生长。Animal Model:Female BALB/c nude mice with MCF-7 cell
Dosage:5 mg/kg, 20 mg/kg and 40 mg/kg
Administration:i.p., daily, 3 weeks
Result:Reduced tumor volume by 11.92%, 26.58% and 39.63%, respectively, when using 5 mg/kg, 20 mg/kg and 40 mg/kg.Significantly induced the expression of Hsp70 and reduced the expression of Akt at 40 mg/kg.

体外研究:
CPUY201112 (0-9 μM, 7 days) 以剂量依赖的方式降低多种癌细胞系的活力, 如 HCT116 结肠细胞、HepG2 肝细胞癌和其他癌细胞。 CPUY201112 (0-2 μM, 24 h) 可以剂量依赖性诱导细胞凋亡。
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