中文名称:

YK 4-279

中文同义词:

4,7-二氯-1,3-二氢-3-羟基-3-[2-(4-甲氧基苯基)-2-氧代乙基]-2H-吲哚-2-酮;RHA与EWS-FLI1结合抑制剂(YK-4-279);YK-4-279游离态;4,7-二氯-3-羟基-3-(2(4-甲氧基苯基)-2-氧代乙基)二氢吲哚-2-酮

英文名称:

YK-4-279

英文同义词:

YK-4-279;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one YK-4-279;YK-4-279;YK 4-279;4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one;CS-1785;2H-Indol-2-one, 4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-;YK-4-279 USP/EP/BP

CAS号:

1037184-44-3

分子式:

C17H13Cl2NO4

分子量:

366.2

EINECS号:

相关类别:

细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;Inhibitors

Mol文件:

1037184-44-3.mol

熔点 

149-151℃

沸点 

608.9±55.0 °C(Predicted)

密度 

1.456

储存条件 

Store at -20° C.

酸度系数(pKa)

10.43±0.20(Predicted)

生物活性

YK-4-279是EWS-FLI1与RNA helicase A (RHA)结合的有效抑制剂。

体外研究

YK-4-279 eliminates cyclin D levels by blocking the interaction of EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. YK-4-279 also specifically inhibits ESFT cell growth and induces apoptosis. YK-4-279 also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion.

体内研究

In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. In mouse model, YK-4-279 selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors.