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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PI3K/mTOR-IN-22 (compound J-33) is a selective dual inhibitor of PI3K and mTOR kinases. Its IC50 for PI3Kα is 400.5 nM and its IC50 for mTOR is 8.2 nM. It can form a stable binding interaction with both kinases [1]. PI3K/mTOR-IN-22 can effectively inhibit the proliferation of MCF-7 human breast cancer cells with an IC50 of 1.5 μM. It can also inhibit the proliferation of H1975, H460 and PC-9 cells with IC50 values of 10.7, 2.3 and 13.5 μM, respectively [1]. PI3K/mTOR-IN-22 (256 μg/mL) has low hemolytic toxicity to sheep erythrocytes with a hemolysis rate of 2.60% [1]. PI3K/mTOR-IN-22 (0.75-1.50 μM; 6-12 h) can induce apoptosis in MCF-7 human breast cancer cells in a concentration-dependent manner, reduce mitochondrial membrane potential and increase intracellular reactive oxygen species (ROS) levels [1]. PI3K/mTOR-IN-22 (0.75-1.50 μM; 24 h) can inhibit the in vitro migration of MCF-7 human breast cancer cells in a dose-dependent manner, as shown in wound healing experiments [1]. PI3K/mTOR-IN-22 (0.19-3.00 μM; 14 days) can inhibit the clonogenic ability of MCF-7 human breast cancer cells in a dose-dependent manner [1]. PI3K/mTOR-IN-22 (0.75-6.00 μM) dose-dependently downregulates the phosphorylation of AKT and mTOR in MCF-7 human breast cancer cells and inhibits the PI3K-AKT-mTOR signaling pathway [1].
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| ln Vivo |
PI3K/mTOR-IN-22 (compound J-33) (75 mg/kg; orally; every other day; 23 days) showed strong in vivo antitumor activity in BALB/c nude mice carrying MCF-7 xenografts, with a tumor inhibition rate of 44.9%[1].
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| Cell Assay |
Cell migration assay [1]
Cell Types: MCF-7 human breast cancer cells Tested Concentrations: 0.75, 1.50 μM Incubation Duration: 24 hours Experimental Results: Compared with the control group, the wound healing rate of cells treated with 0.75 μM was significantly reduced. Compared with the control group, the wound healing rate of cells treated with 1.50 μM was also significantly reduced. The inhibitory effect increased with increasing concentration. Immunofluorescence [1] Cell Types: MCF-7 human breast cancer cells Tested Concentrations: 0.75, 1.50 μM Incubation Duration: 6-12 hours Experimental Results: AO red/green fluorescence ratio increased. JC-1 red/green fluorescence ratio increased. DCFH-DA fluorescence intensity increased. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice with breast cancer (female, 4-6 weeks old, athymic, injected with MCF-7 cells) [1]
Doses: 75 mg/kg Route of Administration: Oral; every other day; for 23 days Experimental Results: Tumor inhibition rate reached 44.9%. Significantly reduced phosphorylation levels of AKT Ser473 site and mTOR in tumor tissue. Blocked the PI3K-AKT-mTOR signaling pathway. Upregulated pro-apoptotic proteins Bax and Caspase-3. Downregulated anti-apoptotic proteins Bcl-2 and proliferation marker Ki-67. Induced tumor cell apoptosis (increased number of TUNEL-positive cells). H&E staining of mouse tissues showed no obvious organ damage. |
| References |
| Molecular Formula |
C28H34N8O6S
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|---|---|
| Molecular Weight |
610.68
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(OC)C1=CC=C(NC(NC2=CC=C(C3=NC(NC4CCN(S(=O)(C)=O)CC4)=NC(N5CCOCC5)=N3)C=C2)=O)C=C1
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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 | 1.6375 mL | 8.1876 mL | 16.3752 mL | |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2750 mL | |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6375 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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