501698-03-9
501698-03-9 结构式
基本信息
中文别名
化合物GDP366化合物 T11383
1-(4-(4-氨基噻吩并[2,3-D]嘧啶-5-基)苯基)-3-(间甲苯基)脲
英文别名
GDP366GDP366
GDP-366
GDP 366
Urea, N-[4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl]-N'-(3-methylphenyl)-
物理化学性质
熔点227-228 °C(Solv: ethanol (64-17-5))
沸点538.5±50.0 °C(Predicted)
密度1.423±0.06 g/cm3(Predicted)
储存条件Keep in dark place,Sealed in dry,2-8°C
溶解度DMSO:62.5(Max Conc. mg/mL);166.47(Max Conc. mM)
酸度系数(pKa)14.22±0.70(Predicted)
形态Solid
颜色Light yellow to yellow
常见问题列表
生物活性
GDP366 是 survivin 和 Op18 的双重抑制剂，抑制癌细胞生长，诱导细胞衰老和有丝分裂突变。靶点
Survivin
Op18
体外研究
GDP366 potently and selectively inhibits the expression of both survivin and Op18. GDP366 decreass both the mRNA and protein levels of survivin and Op18. This inhibitory effect is not dependent on the status of p53 and p21 although GDP366 potently increases p53 and p21 levels. GDP366 significantly inhibits the growth of tumor cells in vitro and in vivo (nude mouse model) without rapid induction of apoptosis. GDP366 induces polyploidy in multiple types of cancer cell lines. GDP366 increases chromosomal instability, and induces cellular senescence by inhibiting telomerase activity.