产品
编 号:F755726
分子式:C15H13NO5S
分子量:319.33
产品类型
结构图
CAS No: 2764598-01-6
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产品详情
生物活性:
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 μM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis.
体内研究:
MMP2-IN-1 (100 mg/kg, 150 mg/kg, 200 mg/kg, 250 mg/kg; IP, single) causes 0%, 30%, 50% and 60% mortality rate at dosing 100 mg/kg, 150 mg/kg, 200 mg/kg and 250 mg/kg respectively.MMP2-IN-1 (10 mg/kg; IP, daily, for 14 days) significantly inhibits tumor growth in metastatic 4T1 murine breast cancer model.Animal Model:Kunming mice (n = 10, half male and half female)
Dosage:100 mg/kg, 150 mg/kg, 200 mg/kg, 250 mg/kg
Administration:IP, single
Result:No mortality occurred after administration of 100 mg/kg, and the mortality rate was 30%, 50% and 60% at dosing 150 mg/kg, 200 mg/kg, 250 mg/kg respectively.
Animal Model:Orthotopic 4T1 tumor-bearing mice
Dosage:10 mg/kg
Administration:IP, daily, for 14 days
Result:Significantly inhibited tumor growth in metastatic 4T1 murine breast cancer model.
体外研究:
MMP2-IN-1 (compound 4a) (0-10 μM; 74 hours) exhibits IC50 values of 0.07 μM, 0.11 μM, and 0.18 μM against MDA-MB-231, A549, and HeLa cancer cells, respectively, and over 10 μM in Hep 5G cells.MMP2-IN-1 (10 μM; 24 hours) induces cell cycle arrest in the S phase.MMP2-IN-1 (0.01 μM, 0.1 μM, 1 μM and 10 μM; 24 hours) induces a dose-dependent increment in early-and late-stage apoptosis of MDA-MB-231 cells, and increased the early-stage apoptosis percentage from 4.66% to 10.9% at 10 μM.