| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
JS04 (72 hours) effectively inhibited the proliferation of H1975 and A549 non-small cell lung cancer (NSCLC) cells, with IC50 values of 8.11 μM and 11.58 μM, respectively; at the same time, the compound showed good safety against human Hs27 fibroblasts, with a selectivity index of 2.52 [1]. JS04 (10-20 μM; 48 hours) induced apoptosis in H1975 cells in a dose-dependent manner [1]. JS04 (10-20 μM; 48 hours) induced cell cycle arrest in the G2/M phase of H1975 cells [1]. JS04 (72 hours) could simultaneously activate the intrinsic apoptosis pathway (downregulating the expression of BCL-2, BCL-xL and Survivin) and the extrinsic apoptosis pathway (upregulating the expression of TRAIL R2/DR5) [1].
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|---|---|
| ln Vivo |
JS04 (6.25–100 μM; immersion treatment; continuous administration; from 5.5 to 6 hours post-fertilization to 96 hours post-fertilization) showed good acute safety in zebrafish (Danio rerio) embryos [1].
|
| Cell Assay |
Apoptosis Analysis [1]
Cell Types: H1975 non-small cell lung cancer cells Tested Concentrations: 10 and 20 μM Incubation Duration: 48 hours Experimental Results: 74% of total apoptosis was induced at a concentration of 20 μM. The apoptosis level at a concentration of 10 μM was lower than that at 20 μM, as evidenced by the reduction in the number of viable cells. Cell cycle analysis [1] Cell Types: H1975 non-small cell lung cancer Tested Concentrations: 10 and 20 μM Incubation Duration: 48 hours Experimental Results: At 20 μM, the number of cells in the G2/M phase increased by about 3 to 4 times (35% of the cells were in the G2/M phase), while the number of cells in the G0/G1 phase decreased. |
| Animal Protocol |
Animal/Disease Models:AB-WT (fertilized egg) [1]
Doses: 6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM Route of Administration: Immersion; Continuous administration; 5.5–6 hpf to 96 hpf Experimental Results: 100 μM and 96 hpf resulted in 100% embryo mortality. Mortality rates at 6.25, 12.5, and 25 μM concentrations were all below 20% at all time points. |
| References |
| Molecular Formula |
C20H23CLN6
|
|---|---|
| Molecular Weight |
382.89
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CNC1=NC(NC2=CC=C(C=C2)N3CCN(CC3)C)=NC4=CC(Cl)=CC=C41
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.6117 mL | 13.0586 mL | 26.1172 mL | |
| 5 mM | 0.5223 mL | 2.6117 mL | 5.2234 mL | |
| 10 mM | 0.2612 mL | 1.3059 mL | 2.6117 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.