CDK1-IN-7是一种有效的CDK1抑制剂 (CDK1/CycBIC50=161.2 nM)，具有潜在的抗增殖活性以及对肿瘤组织有选择性。CDK1-IN-7 通过凋亡内在途径以 p53 依赖的方式诱导细胞凋亡 (Apoptosis)。CDK1-IN-7 是一种潜在的靶向抗肿瘤药物。
| 生物活性 | CDK1-IN-7 is a potentCDK1inhibitor (CDK1/CycBIC50=161.2 nM) with potential antiproliferative activity and selectivity forcancertissues. CDK1-IN-7 inducesapoptosisin p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent[1]. |
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体外研究
(In Vitro) | CDK1-IN-7 (compound 7a) (10 μM, 48 hours) has the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes[1].
CDK1-IN-7 (0.1-100 μM, 48 hours) has better selectivity for cancer cells over normal cell lines (IC50of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8)[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) has a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) can cause cell death mainly through apoptosis rather than necrosis and confirmed that its activity is more selective to cancerous cells than normal cells[1].
CDK1-IN-7 (6.28 μM; 48 hours) induce apoptosis in p53 dependent manner through the intrinsic apoptotic pathway in HCT-116 cells[1].
Cell Proliferation Assay | Cell Line: | 60 human cancer cell lines (LOX IMVI, IGROV1, A498, COLO205 et al.)[1] | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | Had the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes. |
Cell Cytotoxicity Assay | Cell Line: | HCT-116 and WI-38 cells[1] | | Concentration: | 0.1-100 μM | | Incubation Time: | 48 hours | | Result: | Had better selectivity for cancer cells over normal cell lines (IC50of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8). |
Cell Cycle Analysis | Cell Line: | HCT-116 and WI-38 cells[1] | | Concentration: | 17.7 μM in WI-38 and 6.28 μM in HCT-116 | | Incubation Time: | 48 hours | | Result: | Exerted a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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