1151813-61-4
中文名稱
KSI-3716
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T11783 英文別名
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]-
物理化學(xué)性質(zhì)
沸點532.8±50.0 °C(Predicted)
密度1.675±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 5 mg/mL (11.73 mM)
酸度系數(shù)(pKa)-2.74±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to khaki
常見問題列表
生物活性
KSI-3716 是一種有效的 c-Myc 抑制劑，可阻斷 c-MYC/MAX 與靶基因啟動子的結(jié)合。KSI-3716 是一種有效的膀胱內(nèi)化療劑，可用于膀胱癌的研究。靶點
c-Myc
體外研究
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.
體內(nèi)研究
Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity.