KSI-3716

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.

Product information

CAS Number: 1151813-61-4

Molecular Weight: 426.09

Formula: C17H11BrCl2N2O2

Chemical Name: 3-acetyl-8-bromo-5-chloro-2-[(4-chlorophenyl)amino]-1, 4-dihydroquinolin-4-one

Smiles: CC(=O)C1=C(NC2=C(C(Cl)=CC=C2Br)C1=O)NC1C=CC(Cl)=CC=1

InChiKey: URUPDOIKTMCJNA-UHFFFAOYSA-N

InChi: InChI=1S/C17H11BrCl2N2O2/c1-8(23)13-16(24)14-12(20)7-6-11(18)15(14)22-17(13)21-10-4-2-9(19)3-5-10/h2-7H,1H3,(H2,21,22,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

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

References:

1. 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.

Products are for research use only. Not for human use.