AM9928
AM9928 is a monoacylglycerol lipase (MAGL) inhibitor with IC50 and Ki values of 8.9 nM and 7.3 nM, respectively. AM9928 blocks the adhesion and migration of triple-negative breast cancer (TNBC) cells, and inhibits the secretion of IL-6, IL-8 and VEGF-A by TNBC cells. AM9928 suppresses the activation of human brain microvascular endothelial cells (HBMECs) induced by TNBC-derived exosomes, and reduces the secretion of IL-8 and VEGF-A by HBMECs. AM9928 attenuates changes in blood-brain barrier permeability, inhibits tumor growth in the mammary fat pad, and reduces brain colonization of TNBC. AM9928 can be used in studies related to triple-negative breast cancer.
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- CAS No.: 1869033-49-7
- Formule: C24H20N4O2
- Masse moléculaire:396.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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IL-6 |
IL-8 |
AM9928 (100 ng/mL; 10-30 min) blocks adhesion of MDA-MB-BrM2 TNBC cells to HBMEC monolayers at 10 and 30 minutes[1].
AM9928 (100 ng/mL; 5 h) significantly inhibits transmigration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across HBMEC monolayers[1].
AM9928 (250 nM; 72 h) significantly inhibits secretion of IL-6, IL-8, and VEGF-A from MDA-MB-231 and MDA-MB-BrM2 TNBC cells[1].
AM9928 (250 nM; 24 h) alters MDA-MB-231 and MDA-MB-BrM2 TNBC cells to produce exosomes that significantly inhibit IL-8 and VEGF-A secretion from activated HBMECs[1].
AM9928 (range of concentrations; 15 min pre-incubation, 4 hr reaction) inhibits truncated rat fatty acid amide hydrolase (ΔTM rFAAH) with IC50 values of 23 nM and 27 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines)
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Concentration:100 ng/mL
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Incubation Time:5 h
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Result:Significantly inhibited transmigration of MDA-MB-231 and MDA-MB-BrM2 TNBC cells across HBMEC monolayers by approximately 50%.
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Cell Line:MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines)
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Concentration:250 nM
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Incubation Time:72 h
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Result:Reduced IL-6, IL-8 and VEGF-A secretion.
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Cell Line:MDA-MB-231, MDA-MB-BrM2 (human TNBC cell lines), human brain microvascular endothelial cells (HBMECs)
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Concentration:250 nM (TNBC cell treatment)
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Incubation Time:24 h (TNBC cell treatment); 6 h (exosome-HBMEC incubation)
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Result:Reduced HBMEC IL-8 and VEGF-A secretion.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6 weeks old, triple negative breast cancer model via GFP-4T1-BrM5 mammary tumor cell injection into mammary fat pads)[1]
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Dosage:10 mg/kg
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Administration:i.v.; twice weekly; 3 weeks
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Result:Significantly reduced mammary fat pad tumor growth compared to vehicle controls.
Significantly lowered average sum of GFP intensity (measure of brain tumor colonization) compared to vehicle controls.
Significantly decreased BBB permeability (measured by Evans blue dye content in brain tissue) compared to tumor-bearing vehicle controls.
Increased average sum of intensity for ZO-1 tight junction protein expression to 610,920 (vs. 582,096 in vehicle controls).
Increased average sum of intensity for Claudin-5 expression to 681,457 (vs. 518,599 in vehicle controls).
Reduced the number of mice with mammary tumors and brain tumors compared to vehicle controls.
Increased the number of mice alive at day 28 compared to vehicle controls.
Chemical Information
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CAS No. 1869033-49-7
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Masse moléculaire 396.44
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Formule C24H20N4O2
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SMILES
N#CC1=CC(OC(N2CCN(C3C4=C(C5=C3C=CC=C5)C=CC=C4)CC2)=O)=NC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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