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编 号:F042133
分子式:C14H12BrN3OS
分子量:350.23
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM. KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 μM) against various human cell lines.

体内研究:
KGP94 (i.p.; 20 mg/kg; once daily for 3 days) exhibits anti-metastatic and anti-bone resorptive efficacy in a prostate cancer bone metastasis model.Animal Model:NCR nu/nu male mice
Dosage:20 mg/kg
Administration:Intraperitoneal injection; once daily for 3 days
Result:Reduced 65% in metastatic tumor burden and 58% in tumor angiogenesis, improved survival of bone metastases bearing mice.

体外研究:
KGP94 (10 or 20 μM, 24 h) reduces expression of M2 (macrophage) markers (Arginase-1 and CD206) and cells invasion of primary bone marrow-derived macrophages or Raw264.7.KGP94 (25 μM, 24 h) impairs the incasive capacities of both prostate and breat cancer cells by 53% and 88%, respectively.KGP94 (25 μM, 24 h) suppresses secreted CTSL activity by 94% and 92% in PC-3ML and MDA-MB-231, repsectively.
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