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YU238259

CAS No. : 1943733-16-1

MCE 国际站：YU238259

产品活性：YU238259 是一种同源依赖性 DNA 修复 (HDR) 抑制剂，可用于癌症研究。

研究领域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR

作用靶点：DNA-PK

In Vitro: YU238259 is an inhibitor of homology-dependent DNA repair, with no effect on PARP activity. YU238259 shows cytotoxicity in BRCA2-deficient cells, with a low LD₅₀ of 8.5 μM. YU238259 (0-5 μM) causes a potent, dose-dependent decrease in HDR efficiency in U2OS DR-GFP or U2OS EJ5-GFP cells, but with no effect on NHEJ frequency. YU238259 (0-10 μM) exhibits synthetic lethality with loss of frequently mutated tumor suppressors, and shows synergism with radiotherapy (IR) and DNA-damaging chemotherapy that is potentiated by BRCA2 loss.

In Vivo: YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice.

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