1. Apoptosis
  2. c-Myc

KSI-3716 

Cat. No.: HY-12703
Handling Instructions

KSI-3716 is a c-Myc inhibitor.

For research use only. We do not sell to patients.

KSI-3716 Chemical Structure

KSI-3716 Chemical Structure

CAS No. : 1151813-61-4

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  • Biological Activity

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  • References

Description

KSI-3716 is a c-Myc inhibitor.

IC50 & Target

c-Myc[1]

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[1].

In Vivo

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

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3469 mL 11.7346 mL 23.4692 mL
5 mM 0.4694 mL 2.3469 mL 4.6938 mL
10 mM 0.2347 mL 1.1735 mL 2.3469 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Ku19-19 cells are seeded 1 day before drug treatment and treated with KSI-3716 (5, 10, 15, 20, 25 μM) for (12, 24, 48 hours). Cell survival assays are performed to count viable cells[1].

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

Animal Administration
[1]

Mice[1]

[1]The control group is administered solvent and the experimental group (5 tumor bearing mice per group) is administered c-MYC inhibitor KSI-3716 (5 mg/kg) intravesically twice weekly for 3 weeks. Luminescence images are obtained twice weekly[1].

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

References
Molecular Weight

426.09

Formula

C₁₇H₁₁BrCl₂N₂O₂

CAS No.

1151813-61-4

SMILES

ClC1=CC=C(Br)C(NC(NC2=CC=C(Cl)C=C2)=C3C(C)=O)=C1C3=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KSI-3716
Cat. No.:
HY-12703
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KSI-3716

Cat. No.: HY-12703