| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AM9928 (100 ng/mL; 10–30 min) blocked the adhesion of MDA-MB-BrM2 triple-negative breast cancer (TNBC) cells to the human brain microvascular endothelial cell (HBMEC) monolayer at 10 min and 30 min [1]. AM9928 (100 ng/mL; 5 h) significantly inhibited the migration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across the HBMEC monolayer [1]. AM9928 (250 nM; 72 h) significantly inhibited the secretion of IL-6, IL-8 and VEGF-A by MDA-MB-231 and MDA-MB-BrM2 TNBC cells [1]. AM9928 (250 nM; 24 h) induced the production of exosomes from MDA-MB-231 and MDA-MB-BrM2 TNBC cells, which significantly inhibited the secretion of IL-8 and VEGF-A by activated HBMECs [1]. AM9928 (concentration range; 15 min pre-incubation, 4 h reaction) inhibited truncated rat fatty acid amide hydrolase (ΔTM rFAAH) with IC50 values of 23 nM and 27 nM [3].
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|---|---|
| ln Vivo |
AM9928 (10 mg/kg; intravenous injection; twice a week; 3 weeks) significantly reduced the growth of triple-negative breast cancer tumors in the mammary fat pad, reduced blood-brain barrier permeability, and reduced the colonization of brain metastases in BALB/c mice [1].
|
| Cell Assay |
Cell migration assay [1]
Cell Types: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell line) Tested Concentrations: 100 ng/mL Incubation Duration: 5 hours Experimental Results: Significantly inhibited the migration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across the HBMEC monolayer by about 50%. ELISA detection [1] Cell Types: MDA-MB-231, MDA-MB-BrM2 (human TNBC cell line) Tested Concentrations: 250 nM Incubation Duration: 72 hours Experimental Results: IL-6, IL-8 and VEGF-A secretion decreased. ELISA detection [1] Cell Types: MDA-MB-231, MDA-MB-BrM2 (human triple-negative breast cancer cell line), human brain microvascular endothelial cells (HBMEC) Tested Concentrations: 250 nM (triple-negative breast cancer cell treatment) Incubation Duration: 24 hours (triple-negative breast cancer cell treatment); 6 hours (exosome-HBMEC incubation) Experimental Results: HBMEC IL-8 and VEGF-A secretion decreased. |
| Animal Protocol |
Animal/Disease Models:BALB/c (female, 6 weeks old, a triple-negative breast cancer model established by injecting GFP-4T1-BrM5 breast tumor cells into the breast fat pad) [1]
Doses: 10 mg/kg Route of Administration: Intravenous injection; twice a week for 3 weeks Experimental Results: Compared with the vector control group, the growth of breast fat pad tumors was significantly reduced. Compared with the vector control group, the mean sum of GFP intensity (an indicator of brain tumor colonization) was significantly reduced. Compared with the tumor-bearing vector control group, the blood-brain barrier permeability (measured by Evans blue dye content in brain tissue) was significantly reduced. The mean sum of ZO-1 tight junction protein expression intensity increased to 610,920 (582,096 in the vector control group). The mean sum of Claudin-5 expression intensity increased to 681,457 (518,599 in the control group). Compared with the control group, the number of mice with breast tumors and brain tumors was reduced. Compared with the control group, the number of mice surviving on day 28 was increased. |
| References |
|
| Molecular Formula |
C24H20N4O2
|
|---|---|
| Molecular Weight |
396.44
|
| CAS # |
1869033-49-7
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
N#CC1=CC(OC(N2CCN(C3C4=C(C5=C3C=CC=C5)C=CC=C4)CC2)=O)=NC=C1
|
| 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 | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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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