1151813-61-4
中文名称
KSI-3716
英文名称
3-acetyl-8-bromo-5-chloro-2-(4-chloroanilino)-1H-quinolin-4-one
CAS
1151813-61-4
分子式
C17H11BrCl2N2O2
分子量
426.09
MOL 文件
1151813-61-4.mol
![1151813-61-4 结构式](/CAS/20180601/GIF/1151813-61-4.gif)
基本信息
中文别名
化合物 T11783 英文别名
KSI-37163-acetyl-8-bromo-5-chloro-2-(4-chloroanilino)-1H-quinolin-4-one
4(1H)-Quinolinone, 3-acetyl-8-bromo-5-chloro-2-[(4-chlorophenyl)amino]-
物理化学性质
沸点532.8±50.0 °C(Predicted)
密度1.675±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 5 mg/mL (11.73 mM)
酸度系数(pKa)-2.74±0.20(Predicted)
形态Solid
颜色Light yellow to khaki
常见问题列表
生物活性
KSI-3716 是一种有效的 c-Myc 抑制剂,可阻断 c-MYC/MAX 与靶基因启动子的结合。KSI-3716 是一种有效的膀胱内化疗剂,可用于膀胱癌的研究。靶点
c-Myc
体外研究
KSI-3716 blocks c-MYC/MAX from forming a complex with target gene promoters. KSI-3716 effectively blocks complex formation in a dose dependent manner (IC 50 =0.84 μM). c-MYC mediated transcriptional activity is inhibited by KSI-3716 at concentrations as low as 1 μM. The expression of c-MYC target genes, such as cyclin D2, CDK4 and hTERT, is markedly decreased. KSI-3716 exerts cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis.
体内研究
Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity.