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| Targets |
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| ln Vitro |
Target gene promoters and c-MYC/MAX are unable to form a complex due to KSI-3716. In a dose-dependent manner, KSI-3716 efficiently inhibits the formation of complexes (IC50=0.84 μM). KSI-3716 suppresses c-MYC-mediated transcriptional activity at as low as 1 μM concentration. Significant reductions were observed in the expression of c-MYC target genes, including cyclin D2, CDK4, and hTERT. By causing cell cycle arrest and death in bladder cancer cells, KSI-3716 has cytotoxic effects [1].
In vitro, KSI-3716 blocks the binding of c-MYC/MAX to target gene promoters with an IC₅0 of 0.84 microM. The compound suppresses c-MYC-mediated transcriptional activity at concentrations as low as 1 microM, significantly reducing the expression of c-MYC target genes including cyclin D2, CDK4, and hTERT. KSI-3716 exerts cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis. The compound has been shown to be an effective intravesical chemotherapeutic agent for bladder cancer, providing a targeted approach to treating this malignancy. KSI-3716 demonstrates concentration-dependent inhibition of c-MYC activity and cancer cell growth. |
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| ln Vivo |
With little systemic toxicity, intravenous injection of KSI-3716 at a dose of 5 mg/kg can dramatically limit tumor development [1].
In vivo, KSI-3716 is used as an intravesical chemotherapeutic agent for bladder cancer. Intravesical administration delivers the compound directly to the bladder lumen, maximizing local drug concentration while minimizing systemic exposure and toxicity. In preclinical models, KSI-3716 has demonstrated antitumor activity against bladder cancer. The compound induces cell cycle arrest and apoptosis in tumor cells, leading to reduced tumor growth. The c-MYC inhibition by KSI-3716 represents a promising strategy for bladder cancer treatment, particularly for patients who are refractory to conventional therapies. |
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| Enzyme Assay |
In vitro biochemical assays for KSI-3716 involve assessing the inhibition of c-MYC/MAX binding to DNA. Electrophoretic mobility shift assays (EMSA) are performed using recombinant c-MYC and MAX proteins and a fluorescently or radioactively labeled oligonucleotide containing the E-box DNA sequence (CACGTG). Varying concentrations of KSI-3716 are incubated with the proteins before adding the DNA probe. The protein-DNA complexes are resolved on native polyacrylamide gels and visualized. IC₅0 values for inhibition of complex formation are determined. Alternatively, fluorescence polarization or surface plasmon resonance assays can be used to measure the binding of c-MYC/MAX to DNA in the presence of the compound.
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| ADME/Pharmacokinetics |
KSI-3716 (CAS#: 1151813-61-4) has molecular formula C1₇H11BrCl2N2O2 and molecular weight 426.09. The compound is a potent c-Myc inhibitor that blocks c-MYC/MAX binding to target gene promoters, suppressing c-MYC-mediated transcription. KSI-3716 exerts cytotoxic effects on bladder cancer cells by inducing cell cycle arrest and apoptosis. The compound is an effective intravesical chemotherapeutic agent for bladder cancer. KSI-3716 is a research chemical for laboratory use only. Storage should be in a cool, dry place. The compound is soluble in DMSO and is intended for research use only, not for human therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicological information for KSI-3716 is limited as the compound is a research chemical. Based on its mechanism of c-MYC inhibition, potential toxicities may include effects on rapidly proliferating tissues such as the gastrointestinal tract, bone marrow, and skin, which are typical of anti-proliferative agents. The compound should be handled with standard laboratory precautions including the use of personal protective equipment and working in a well-ventilated area. Avoid inhalation, ingestion, and skin contact. The compound should be stored in a cool, dry place and disposed of according to institutional guidelines for chemical waste.
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| References | ||
| Additional Infomation |
KSI-3716 (CAS#: 1151813-61-4) is a potent c-Myc inhibitor that blocks c-MYC/MAX binding to target gene promoters, suppressing c-MYC-mediated transcriptional activity. c-MYC is a well-established oncogene that is overexpressed in many human cancers and is a promising therapeutic target. KSI-3716 is being developed as an intravesical chemotherapeutic agent for bladder cancer. The compound induces cell cycle arrest and apoptosis in bladder cancer cells. KSI-3716 represents a novel approach to targeting c-MYC in cancer therapy. As of the current date, KSI-3716 remains a preclinical research compound and has not been approved for clinical use. The compound is supplied for research use only.
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| Molecular Formula |
C17H11BRCL2N2O2
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| Molecular Weight |
426.091441392899
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| Exact Mass |
423.938
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| CAS # |
1151813-61-4
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| Related CAS # |
KSI-3716-d4
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| PubChem CID |
44565901
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
5.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1=CC=C(C2C(C(C(C)=O)=C(NC3C=CC(=CC=3)Cl)NC=21)=O)Cl
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| InChi Key |
URUPDOIKTMCJNA-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-acetyl-8-bromo-5-chloro-2-(4-chloroanilino)-1H-quinolin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~11.73 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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