KSI-3716


Catalog No. Size PriceQuantity
M12760-2 2mg solid $170
M12760-10 10mg solid $555

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: ≥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.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed