1943733-16-1
中文名稱
YU238259
英文名稱
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
2024/12/18 10:22:11
1943733-16-1 結(jié)構(gòu)式
基本信息
中文別名
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
英文別名
YU238259YU-238259
YU 238259
Benzamide, N-[2-(5-chloro-2-pyridinyl)ethyl]-4-[[[(4-methoxyphenyl)sulfonyl]amino]methyl]-
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
密度1.323±0.06 g/cm3(Predicted)
儲存條件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
酸度系數(shù)(pKa)11.46±0.50(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white
常見問題列表
生物活性
YU238259 是一種同源依賴性 DNA 修復(fù) (HDR) 抑制劑，可用于癌癥研究。靶點(diǎn)
HDR
體外研究
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.
體內(nèi)研究
YU238259 (3 mg/kg, i.p.) inhibits the growth of BRCA2-deficient tumor xenografts in nude mice.