生物活性 | |||
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描述 | BQU57 is a Ral inhibitor which can reduced the activation of RalA without effect on the binding of GTP or GDP to RalA. Treatment with BQU57 at concentration<10μM for 2-4 weeks dose-dependently inhibited the anchorage-independent colony formation of Ral-dependent lines, H2122 and H358. Administration of BQU57 at doses of 20mg/kg or 50mg/kg, i.p., inhibited the growth of H2122 tumour xenografts, with decreased activity of RalA and RalB (measured using the respective pull-down assay for each GTPase) in tumor. | ||
作用机制 | BQU57 may bind to the guanine nucleotide binding pocket in RalA–GDP.[1] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.99mL 0.60mL 0.30mL |
14.96mL 2.99mL 1.50mL |
29.91mL 5.98mL 2.99mL |
参考文献 |
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