NKP-1339 (IT-139; KP-1339) 是针对实体癌开发的一流钌抗癌试剂，副作用小。NKP-1339 通过线粒体途径诱导 G2/M 细胞周期停滞，DNA 合成阻断 (DNA synthesis) 和诱导细胞凋亡 (apoptosis)。NKP-1339 具有很高的肿瘤靶向潜力，与血清蛋白 (serum proteins) 如白蛋白和转铁蛋白强烈结合，并在还原性肿瘤环境中激活。
NKP-1339 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC
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values of 45-200 μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC
50
value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC
50
values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively.
NKP-1339 (0-150 μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either.
NKP-1339 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment.
Cell Viability Assay
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Cell Line:
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Hepatoma, Melanoma, Lung cancer and Colon cancer cell lines
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Concentration:
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0 μM, 50 μM, 100 μM, 150 μM and 200 μM
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Incubation Time:
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72 hours
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Result:
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Has anti-cancer activity in diverse malignant tumour cell types.
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Apoptosis Analysis
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Cell Line:
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Hep3B cells
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Concentration:
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0 μM, 75 μM, 150 μM
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Incubation Time:
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72 hours
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Result:
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Promoted cell apoptosis as a concentration manner.
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Western Blot Analysis
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Cell Line:
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Hep3B cells
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Concentration:
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0 μM, 75 μM, 150 μM
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Incubation Time:
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72 hours
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Result:
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Increased p-STAT3 and p-CREB expression in cells without sorafenib cotreatment.
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