KSI-3716 is a potent c-Myc inhibitor that blocks c-MYC/MAX binding to target gene promoters. KSI-3716 is an effective intravesical chemotherapy agent for bladder cancer.
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 (IC50=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.
分子式
C17H11BrCl2N2O2
分子量
426.09
CAS号
1151813-61-4
运输条件
Room temperature in continental US; may vary elsewhere.