| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Anticancer agent 320 (compound 6g) (3.125-50 μM) inhibited the activity of MCF7, A549 and HCT116 cancer cells, with IC50 values of 0.89, 1.02 and 1.29 μM, respectively, while exhibiting extremely low toxicity to MRC-5 cells (≥100 μM) [1]. Anticancer agent 320 (0.89-1.29 μM; 72 h) induced G1 phase arrest in HCT116 and A549 cells and G2 phase arrest in MCF7 cells [1]. Anticancer agent 320 (0.89-1.29 μM; 72 h) induced DNA double-strand breaks in A549 and HCT116 cells, but had no significant effect on DNA damage in MCF7 cells [1]. Anticancer drug 320 (0.89-1.29 μM; 72 h) can effectively induce early apoptosis in A549 cells and slightly induce early apoptosis in HCT116 and MCF7 cells [1]. Anticancer drug 320 (0.89-1.29 μM; 72 h) inhibits the growth of three-dimensional spheroids in A549 cells and inhibits the initial spheroid formation in MCF7 cells [1]. Anticancer drug 320 (0.89-1.29 μM; 72 h) inhibits the long-term colony formation of A549, HCT116 and MCF7 cells, with the strongest inhibitory effect on HCT116 cells [1]. Anticancer drug 320 exhibits good binding interactions with key cancer-related proteins, with the highest affinity for MAPK8 (docking score of -7.872 kcal/mol) and the binding free energy of MM-GBSA (-55.11 kcal/mol) [1]. The anticancer drug 320 can reduce the membrane potential of A549, HCT116 and MCF7 cells[1].
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|---|---|
| Cell Assay |
Cell cycle analysis [1]
Cell Types: A549, HCT116, MCF7 Test concentrations: 0.89 (MCF7), 1.02 (A549) and 1.29 μM (HCT116) Incubation Duration: 72 hours Experimental Results: In HCT116 cells, the proportion of cells in G1 phase increased to 43.1%, and the proportion of cells in S phase decreased to 31.1%, indicating G1 phase arrest. In A549 cells, the proportion of cells in G1 phase increased to 62.6%, and the proportion of cells in S phase decreased to 18.8%, indicating G1 phase arrest. In MCF7 cells, the percentage of cells in the G1 phase increased to 69.6%, and the percentage in the G2 phase increased significantly to 30.3%, indicating that it has a unique G2 phase accumulation feature, which is different from the G1 phase arrest observed in other cell lines. Apoptosis Analysis [1] Cell Types: A549, HCT116, MCF7 Tested Concentrations: 0.89 μM (MCF7), 1.02 μM (A549), and 1.29 μM (HCT116) Incubation Duration: 72 hours Experimental Results: 77.83% of A549 cells underwent early apoptosis, with only 10.07% surviving. 14.98% of HCT116 cells underwent early apoptosis, with 70.58% surviving. 23.1% of MCF7 cells underwent early apoptosis. |
| References |
| Molecular Formula |
C20H20FN3O3
|
|---|---|
| Molecular Weight |
369.39
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CCC(N1C(C(C(NCC2=NC=CC=C2)=O)=C(C3=CC(F)=CC=C31)O)=O)C
|
| 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 | 2.7072 mL | 13.5358 mL | 27.0717 mL | |
| 5 mM | 0.5414 mL | 2.7072 mL | 5.4143 mL | |
| 10 mM | 0.2707 mL | 1.3536 mL | 2.7072 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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