产品
编 号：F756648
分子式：C24H25N9
分子量：439.52
分子式：C24H25N9
分子量：439.52
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CAS No: 2890819-31-3
产品详情
生物活性：
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage.
体内研究：
Mps1-IN-5 (30, 60 mg/kg; p.o.; daily for 15 days) 在乳腺癌模型中抑制肿瘤生长而无明显毒性。Animal Model:6-8 weeks, female BALB/C mice (4T1-luc mouse xenograft model)
Dosage:30, 60 mg/kg
Administration:P.o.; daily for 15 days
Result:Significantly suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys.
体外研究：
Mps1-IN-5 (compound 12) (0-10 μM,24, 48, 72 h) 以时间依赖性方式抑制 MCF-7 和 4T1 细胞的增殖.Mps1-IN-5 (0, 0.5, 1.0, 5.0 μM; 24, 48 h) 在 MCF-7 和 4T1 细胞中以剂量依赖性方式诱导细胞凋亡和胞周期停滞在 G2/M 期 .Mps1-IN-5 (0, 0.03, 0.1, 1, 3 μM; 2 h) 抑制 Mps1 的磷酸化并诱导 DNA 损伤。
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage.
体内研究：
Mps1-IN-5 (30, 60 mg/kg; p.o.; daily for 15 days) 在乳腺癌模型中抑制肿瘤生长而无明显毒性。Animal Model:6-8 weeks, female BALB/C mice (4T1-luc mouse xenograft model)
Dosage:30, 60 mg/kg
Administration:P.o.; daily for 15 days
Result:Significantly suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys.
体外研究：
Mps1-IN-5 (compound 12) (0-10 μM,24, 48, 72 h) 以时间依赖性方式抑制 MCF-7 和 4T1 细胞的增殖.Mps1-IN-5 (0, 0.5, 1.0, 5.0 μM; 24, 48 h) 在 MCF-7 和 4T1 细胞中以剂量依赖性方式诱导细胞凋亡和胞周期停滞在 G2/M 期 .Mps1-IN-5 (0, 0.03, 0.1, 1, 3 μM; 2 h) 抑制 Mps1 的磷酸化并诱导 DNA 损伤。
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