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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Jeong KC, et al. Intravesical instillation of c-MYC inhibitor KSI-3716 suppresses orthotopic bladder tumor growth. J Urol. 2014 Feb;191(2):510-8.  [Content Brief]