Description
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: ≥12 months 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:
- 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.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.