产品
编 号:F281393
分子式:C23H20N2O2
分子量:356.42
产品类型
结构图
CAS No: 2242470-43-3
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产品详情
生物活性:
DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
体内研究:
DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice.Animal Model:Nude mice (6-weeks-old) with H929 775 cells
Dosage:50 mg/kg
Administration:Intraperitoneal injection; every day for 14 days
Result:Significantly reduced the growth of MM cells-induced tumors.
体外研究:
DCZ0415 (10, 20 μM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation. DCZ0415 (1.25-40 μM; 72 hours) induces a significant dose-dependent decrease of viability in MM cells. DCZ0415 (10, 20 μM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death. DCZ0415 (10, 20 μM; 24 hours) induces a significant accumulation in G0/G1 MM cells. DCZ0415 (10 μM; 48 hours) decreases the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells. DCZ0415 has IC50s of 1.0–10 μM in CalcuSyn in MM cell lines. DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells.