eALM1137
eALM1137 is a mTOR inhibitor with an IC50 of 4.8 nM. eALM1137 mediates dual inhibition of the mTORC1 and mTORC2 signaling pathways, and inhibits DNA-PK (IC50=77 nM). eALM1137 exhibits antiproliferative and cytostatic activities, and induces G1 cell cycle arrest. eALM1137 is applicable to the research of glioblastoma multiforme.
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- Formule: C22H26N8O3
- Masse moléculaire:450.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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mTORC1 |
mTORC2 |
eALM1137 (0.1-1000 nM; 5 days) potently inhibits U87-MG glioblastoma cell proliferation with an EC50 of 5.1 nM after 5 days of treatment[1].
eALM1137 (0.1-1000 nM; 5 days) potently inhibits T98G glioblastoma cell proliferation with an EC50 of 11 nM after 5 days of treatment[1].
eALM1137 (3 nM, 10 nM, 30 nM, 100 nM, 300 nM) dose-dependently inhibits mTORC1 and mTORC2 signaling in U87-MG and T98G glioblastoma cells, with marked reduction of phosphorylated S6 and Akt at concentrations ≥30 nM[1].
eALM1137 (10-8-10-5 M; 3 days) potently inhibits NPE glioblastoma stem cell proliferation with an EC50 of 85 nM after 3 days of treatment, exerting cytostatic rather than cytotoxic effects[1].
eALM1137 (300 nM; 24 h) inhibits mTORC1 and mTORC2 signaling in NPE glioblastoma stem cells after 24 h of treatment at 300 nM, while inducing compensatory activation of the RAF-MEK-ERK pathway[1].
eALM1137 (0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM; 3 days) induces dose-dependent G1-phase cell cycle arrest in E21 patient-derived glioblastoma stem cells after 3 days of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87-MG glioblastoma multiforme cells
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Concentration:0.1-1000 nM
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Incubation Time:5 days
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Result:Suppressed U87-MG cell proliferation with an EC50 of 5.1 nM.
Showed stronger potency than reference compound sapanisertib (EC50=7.5 nM).
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Cell Line:E21 patient-derived mesenchymal glioblastoma stem cells expressing FUCCI cell cycle reporter
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Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
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Incubation Time:3 days
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Result:Induced a strong G1-phase cell cycle arrest in a dose-dependent manner.
Caused significant increases in the percentage of G1-phase cells relative to DMSO control at all tested concentrations.
Chemical Information
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Masse moléculaire 450.49
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Formule C22H26N8O3
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SMILES
O=C(N1CCC(CN2N=C(C3=CC=C(OC(N)=N4)C4=C3)C5=C(N)N=CN=C52)CC1)OC(C)C
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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)
- eALM1137
- eALM 1137
- eALM-1137
- mTOR
- Ribosomal S6 Kinase (RSK)
- Akt
- DNA-PK
- mechanistic target of rapamycin
- U87-MG glioblastoma cell
- glioblastoma multiforme
- mTORC1
- NPE glioblastoma stem cell
- E21 patient-derived glioblastoma stem cell
- mTORC2
- T98G glioblastoma cell
- G1 cell cycle arrest
- RAF-MEK-ERK pathway
- Inhibitor
- inhibitor
- inhibit