生物活性 | |||
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描述 | YU238259 is a novel DNA double-strand break repair inhibitor exhibiting potent synthetic lethality in the setting of DNA damage response and DNA repair defects. YU238259 specifically inhibits homology-dependent DNA repair, but not non-homologous end-joining, in cell-based GFP reporter assays at concentration of 5μM. Treatment with YU238259 was not only synergistic with ionizing radiation, etoposide, and PARP inhibition, but this synergism was heightened by BRCA2 deficiency. Also it significantly delayed growth of BRCA2-deficient human tumor xenografts in nude mice through administration at dose of 3mg/kg, i.p., 3 days per week for 12 doses, even in the absence of concomitant DNA-damaging therapy. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.87mL 2.17mL 1.09mL |
21.74mL 4.35mL 2.17mL |
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