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CDK1-IN-1
CDK1-IN-7是一种有效的 CDK1 抑制剂 (CDK1/CycB IC50=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。
CDK1-IN-1 Chemical Structure
CAS No. : 2761858-59-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent[1].
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| IC50 & Target |
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CDK1/cycB
161.2 nM (IC50)
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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 (IC50 of 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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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 (IC50 of 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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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Elgiushy HR, et al. Identification of a promising hit from a new series of pyrazolo[1,5-a]pyrimidine based compounds as a potential anticancer agent with potent CDK1 inhibitory and pro-apoptotic properties through a multistep in vitro assessment [published online ahead of print, 2022 Jan 29]. Bioorg Chem. 2022;120:105646.
[2]. Gangadevi S, et al. Kobophenol A Inhibits Binding of Host ACE2 Receptor with Spike RBD Domain of SARS-CoV-2, a Lead Compound for Blocking COVID-19. J Phys Chem Lett. 2021;12(7):1793-1802.
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