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8-(4-二苯并噻吩基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮
8-(4-二苯并噻吩基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮

基本信息 产品名称 8-(4-二苯并噻吩基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮
英文名称 8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one  
别名 KU-57788  
CAS 503468-95-9  
分子式 C25H19NO3S  
分子量 413.48800  

物化性质 bp
nD20  
density  
fp  
外观 淡黄色固体  

运输信息
UNNumber  
Class  
PG  
危险性描述  
安全性描述  

用途信息
用途 U-57788(NU7441)是DNA-PK选择性抑制剂,IC50为14  

其它信息 KU-57788(NU7441) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 value of  are 14 nM; 1700, 5000, >100000 and >100000 nM for  mTOR, PI 3K, ATM and ATR respectively; also is a modest inhibitor of BRD4 and BRDT with IC50s of 1 and 3.5 uM respectively.
IC50 value: 14 nM (DNA-PK)[1]; 1/3.5 uM(BRD4/BRDT) [4]
Target: DNA-PK; BRD4/BRDT
in vitro:  NU7441 increased the cytotoxicity of ionizing radiation and etoposide in SW620, LoVo, and V3-YAC cells but not in V3 cells, confirming that potentiation was due to DNA-PK inhibition. NU7441 substantially retarded the repair of ionizing radiation-induced and etoposide-induced DSB. NU7441 appreciably increased G(2)-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells [2]. NU7441 strongly inhibited DNA-PK in cell lines (IC(50) = 0.3 μM) but only weakly inhibited PI3 K (IC(50) = 7 μM). NU7441 caused doxorubicin- and IR-induced DNA DSBs (measured by γ-H2AX foci) to persist and also slightly decreased homologous recombination activity, as assessed by Rad51 foci [3]. NU7441 is a modest inhibitor of BRD4 and BRDT (IC50 = 1 and 3.5 SM, respectively), which establishes a single hydrogen bond in the KAc site through the chromenone oxygen with Asn140 [4].
in vivo: In mice bearing SW620 xenografts, NU7441 concentrations in the tumor necessary for chemopotentiation in vitro were maintained for at least 4 hours at nontoxic doses. NU7441 increased etoposide-induced tumor growth delay 2-fold without exacerbating etoposide toxicity to unacceptable levels [2].


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