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AZ3146

CAS No. : 1124329-14-1

MCE 站：AZ3146

产品活性：AZ3146 是一种有效的选择性的 Mps1 抑制剂，作用于 Mps1^Cat，IC₅₀ 为 35 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：Mps1

In Vitro: In in vitro kinase assays, AZ3146 inhibits human Mps1^Cat with IC₅₀ of ~35 nM. AZ3146 also efficiently inhibits autophosphorylation of full-length Mps1 immunoprecipitated from human cells. TTK specific kinase inhibitor AZ3146 can decrease HCC cell growth. In vitro cell cytotoxicity assays are performed on SMMC-7721 and BEL-7404 cells. IC₅₀s are calculated as being 7.13 μM (BEL-7404) and 28.62 μM (SMMC-7721). Both cells are further treated under the concentration of IC50 for 4 days. Significant inhibitions of cell proliferation are observed. HCT116 cells are cultured for 10 days in 0.8 μM (the GI₅₀) of AZ3146 , then 2 μM AZ3146 for 3 weeks. Sixteen clones are isolated and cell lines generated, named AzR1-16, all of which are resistant to AZ3146-induced cell death in cell viability assays; AzR3 and 4 have a GI₅₀ of approximately 3 μM (4-fold resistance), while the remaining clones have a GI₅₀ of approximately 9 μM (11-fold resistance). When analyzing mitosis by time-lapse microscopy, while 2 μM AZ3146 causes the parental cell line to rapidly exited mitosis in 10 minutes.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Cytoskeleton Compound Library  |  MPI-0479605  |  Mps1-IN-1  |  Mps1-IN-3  |  TC-Mps1-12  |  Mps1-IN-1 dihydrochloride

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