1943733-16-1
中文名称
YU238259
英文名称
YU238259
CAS
1943733-16-1
分子式
C22H22ClN3O4S
分子量
459.95
MOL 文件
1943733-16-1.mol
更新日期
2024/08/14 11:24:10
1943733-16-1 结构式
基本信息
中文别名
化合物YU238259N-(2-(5-氯吡啶-2-基)乙基)-4-((4-甲氧基苯磺酰胺基)甲基)苯甲酰胺
英文别名
YU238259YU-238259
YU 238259
Benzamide, N-[2-(5-chloro-2-pyridinyl)ethyl]-4-[[[(4-methoxyphenyl)sulfonyl]amino]methyl]-
所属类别
生物化工：激动剂抑制剂物理化学性质
密度1.323±0.06 g/cm3(Predicted)
储存条件Inert atmosphere,Room Temperature
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
酸度系数(pKa)11.46±0.50(Predicted)
形态结晶固体
颜色White to off-white
常见问题列表
生物活性
YU238259 是一种同源依赖性 DNA 修复 (HDR) 抑制剂，可用于癌症研究。靶点
HDR
体外研究
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 LD 50 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.
体内研究
YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice.