产品
编 号:F755721
分子式:C23H25FN4O
分子量:392.47
产品类型
结构图
CAS No: 2763840-83-9
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产品详情
生物活性:
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model.
体内研究:
PARP-1-IN-1 (compound Y49) (50 mg/kg/day; p.o.; daily for 18 days) inhibits the growth of MDA-MB-436 tumor in BALB/c nude mice.Animal Model:Female athymic BALB/c nude mice (inoculated MDA-MB-436 cells)
Dosage:50 mg/kg
Administration:p.o., daily for 18 days
Result:Inhibited the growth of MDA-MB-436 tumor significantly, and no significant change in the body weight of PARP-1-IN-1 treated mice.
体外研究:
PARP-1-IN-1 (compound Y49) (48 hours) has effective inhibition on different cancer cells (IC50s of 9.64, 123.5 106.3 μM for MX-1, MCF7 and A548 cells, respectively).PARP-1-IN-1 (2.5-10 μM, 48 hours) successfully inhibits the activity of PARP-1 and reduces the production of PAR in A549 cells, which is dose-dependent to some extent.