CDK1-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

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

CDK1-IN-1 Chemical Structure

CAS No. : 2761858-59-5

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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].

IC50 & Target

CDK1/cycB

161.2 nM (IC50)

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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

465.50

Formula

C27H23N5O3

CAS 号

2761858-59-5

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.

参考文献
  • [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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