| ln Vitro |
PI3K/mTOR-IN-17 (compound 8) exhibited excellent cytotoxicity, with IC50 values of 21.13 μM (WI-38 lung fibroblasts) and 1.39 μM (A549 cells), and a selectivity index of 15.32 [1]. PI3K/mTOR-IN-17 (1.39 μM, 48 h) upregulated the levels of p53 and Bax in A549 cells and downregulated the levels of Bcl-2, EGFR, PI3K and mTOR [1]. PI3K/mTOR-IN-17 (1.39 μM, 48 h) also upregulated the levels of initiating caspase-8 and caspase-9 and executing caspase-3 and caspase-7 in A549 cells [1]. PI3K/mTOR-IN-17 (1.39 μM, 48 h) significantly induced apoptosis in A549 cells by arresting their growth in the G1 phase [1].
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| Cell Assay |
Real-time quantitative PCR[1]
Cell Types: A549 lung cancer cells Tested Concentrations: 1.39 μM Incubation Duration: 48 h Experimental Results: p53 expression was significantly upregulated by 8.38-fold, Bax expression was significantly upregulated by 9.88-fold, and Bcl-2 expression was downregulated by 0.45-fold. EGFR, PI3K and mTOR gene expression were inhibited by 0.42-fold, 0.45-fold and 0.58-fold, respectively. Apoptosis analysis [1] Cell Types: A549 lung cancer cells Tested Concentrations: 1.39 μM Incubation Duration: 48 hours Experimental Results: The overall mortality rate was significantly increased by 21-fold. The total apoptosis rate reached 25.03% (of which late apoptosis accounted for 19.38% and early apoptosis accounted for 5.65%), while the untreated control group was 1.19%. The proportion of cells in G1 phase significantly increased to 80.2%, while the control group was 57.3%, and the proportion of cells in S phase and G2/M phase significantly decreased. ELISA detection [1] Cell Types: A549 lung cancer cells Tested Concentrations: 1.39 μM Incubation Duration: 48 hours Experimental Results: The levels of initiating caspase-8 and 9 were upregulated by nearly 2.2-fold and 1.03-fold, respectively, and the levels of executing caspase-3 and 7 were upregulated by 1.73-fold and 1.34-fold, respectively. |
| References |
| Molecular Formula |
C36H34N4O6
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|---|---|
| Molecular Weight |
618.68
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(N1C2=CC=C(NC(C(C3=CC=CC=C3)N(C4=CC=C(C)C=C4)C(CNC(OC(C)(C)C)=O)=O)=O)C=C2)C5=CC=CC=C5C1=O
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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) |
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 | 1.6163 mL | 8.0817 mL | 16.1634 mL | |
| 5 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL | |
| 10 mM | 0.1616 mL | 0.8082 mL | 1.6163 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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