| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
mTOR 0.002 μM (IC50)
|
|---|---|
| ln Vitro |
Together with rapamycin, CC214-1 (0, 0.1, 1, 2, 5, 10 μM, 8 h; 2 μM, 24 h) inhibits mTORC1 signaling and tumor cell proliferation [1]. Glioblastoma cells are sensitive to growth arrest because of EGFRvIII expression and PTEN loss, which is mediated by CC214-1 (2 μM, 24 h) [1]. In GBM39 cells, CC214-1 (5 μM, 0-48 h) significantly lipidates LC3B-I to LC3B-II isoform and triggers autophagy [1]. CC214-1's IC50 against mTOR is 0.002 μM [2]. T cell activation and the expression of T cell activation markers can be successfully inhibited by CC214-1 (0-10 μM, 4 days) [3].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: glioblastoma Tested Tested Concentrations: 0, 0.1, 1, 2, 5, 10 μM; 2 μM Incubation Duration: 8 h; 24 h Experimental Results: Inhibited mTORC1 signaling in all glioblastoma cell lines tested, potently suppressing rapamycin -resistant 4E-BP1 and mTORC2 signaling. Inhibited mTORC1-dependent 4E-BP1 and S6 phosphorylation in EGFRvIII-expressing glioblastoma cells, as well as blocked glioblastoma cells overexpressing wild-type EGFR. Immunofluorescence[1] Cell Types: glioblastoma Tested Tested Concentrations: 2 μM , 5 μM Incubation Duration: 4 h; 0, 4, 12, 24, 48 h Experimental Results: Induced a transient expression of LC3B-II isoform and the conjugation of Atg12 to Atg5 indicative of the stimulation of the autophagy flux in U87EGFRvIII cell line. Massively lipidated LC3B-I to LC3B-II subtype and induces autophagy in GBM39 cells. Cell Cycle Analysis[3] Cell Types: glioblastoma Tested Tested Concentrations: 0-10 μM Incubation Duration: 4 day Experimental Results: Induced TEE cells in CD4+ and CD8+ T cell subsets . |
| References |
|
| Molecular Formula |
C20H21N7O2
|
|---|---|
| Molecular Weight |
391.43
|
| CAS # |
1021920-32-0
|
| Appearance |
Typically exists as solid at room temperature
|
| 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
|
|---|---|
| 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 | 2.5547 mL | 12.7737 mL | 25.5474 mL | |
| 5 mM | 0.5109 mL | 2.5547 mL | 5.1095 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5547 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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