1037184-44-3
中文名稱
YK 4-279
英文名稱
YK-4-279
CAS
1037184-44-3
分子式
C17H13Cl2NO4
分子量
366.2
MOL 文件
1037184-44-3.mol
更新日期
2024/12/15 19:35:19
1037184-44-3 結(jié)構(gòu)式
基本信息
中文別名
YK-4-279游離態(tài)RHA與EWS-FLI1結(jié)合抑制劑(YK-4-279)
4,7-二氯-3-羥基-3-(2(4-甲氧基苯基)-2-氧代乙基)二氫吲哚-2-酮
4,7-二氯-1,3-二氫-3-羥基-3-[2-(4-甲氧基苯基)-2-氧代乙基]-2H-吲哚-2-酮
英文別名
CS-1785YK-4-279
1037184-44-3
YK-4-279
YK 4-279
YK-4-279 USP/EP/BP
4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one
2H-Indol-2-one, 4,7-dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-
4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one YK-4-279
所屬類別
生物化工：DNA/RNA Synthesis 抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)149-151℃
沸點(diǎn)608.9±55.0 °C(Predicted)
密度1.456
儲(chǔ)存條件Store at -20° C.
溶解度insoluble in H2O; ≥16.35 mg/mL in DMSO; ≥24.25 mg/mL in EtOH with ultrasonic
酸度系數(shù)(pKa)10.43±0.20(Predicted)
形態(tài)粉末
顏色White to off-white
常見問題列表
生物活性
YK-4-279是EWS-FLI1與RNA helicase A (RHA)結(jié)合的有效抑制劑。體外研究
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.體內(nèi)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.