KSI-3716 is a potentc-Mycinhibitor that blocks c-MYC/MAX binding to target gene promoters. KSI-3716 is an effective intravesical chemotherapy agent for bladdercancer^[1].

c-Myc^[1]

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^[1].

Intravesical instillation of KSI-3716 at a dose of 5 mg/kg significantly suppresses tumor growth with minimal systemic toxicity^[1].

426.09

Solid

C₁₇H₁₁BrCl₂N₂O₂

1151813-61-4

Room temperature in continental US; may vary elsewhere.

DMSO : 5 mg/mL(11.73 mM;Need ultrasonic)

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