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编 号:F458900
分子式:C23H22Cl2N4O3
分子量:473.35
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1mg
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生物活性:
RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity.

体外研究:
RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells.RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells.RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC50 value for inhibition of colony formation by RGB-286147 is 57 nM. RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI50 value of RGB-286147 相关抗体:Cell Cycle AnalysisCell Line:HCT116 cells
Concentration:50 nM and 100 nM
Incubation Time:24 or 48 hr
Result:Caused a marked inhibition of DNA replication and induced cell cycle arrest.
Western Blot AnalysisCell Line:HCT116 cells
Concentration:100 nM
Incubation Time:48 hr
Result:Resulted in proteolytic cleavage of PARP.
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