GSK-3β/VEGFR2-IN-1
GSK-3β/VEGFR2-IN-1 is an orally active dual inhibitor of GSK-3β (IC50 = 325 nM) and VEGFR2 (IC50 = 78 nM). GSK-3β/VEGFR2-IN-1 suppresses the phosphorylation of VEGFR2, AKT, MEK and ERK, inhibits human tongue squamous cell carcinoma cells migration and suppresses formation of HUVECs, exhibits low toxicity towards other cancer cells and normal cells, demonstrates significant antitumor efficacy in a CAL27 xenograft mouse model. GSK-3β/VEGFR2-IN-1 can be used for the study of tongue squamous cell carcinoma.
For research use only. We do not sell to patients.
- Formula: C30H31N7O4S
- Molecular Weight:585.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GSK-3β 325 nM (IC50) |
VEGFR2 78 nM (IC50) |
Akt |
MEK |
GSK-3β/VEGFR2-IN-1 (compound 9) inhibits GSK-3β (IC50 = 325 nM, mixtures incubate at room temperature for 30 min) and VEGFR2 (IC50 = 78 nM, mixtures incubate at 28°C for 1 h)[1].
GSK-3β/VEGFR2-IN-1 (1.5 μM) inhibits VEGFR1/Lck (> 90% inhibition) and GSK-3α (67% inhibition) and shows no significant activity against other kinases tested[1].
GSK-3β/VEGFR2-IN-1 (72 h) shows no antiproliferative activity against MDA-MB-231, MDA-MB-468, A549 and CAL27 cells (IC50 > 100 μM) and weak activity against HUVECs (IC50 = 41.3 μM)[1].
GSK-3β/VEGFR2-IN-1 (5-15 μM; 24 h) inhibits CAL27 cells migration and suppresses the phosphorylation of VEGFR2, AKT, MEK and ERK in CAL27 cells[1].
GSK-3β/VEGFR2-IN-1 (10-40 μM; 5 h) inhibits HUVECs tubular network formation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CAL27 cells
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Concentration:5 μM, 10 μM, 15 μM
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Incubation Time:24 h
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Result:Inhibited CAL27 cells migration.
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Cell Line:CAL27 cells
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Concentration:5 μM, 10 μM, 15 μM
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Incubation Time:24 h
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Result:Suppressed the phosphorylation of VEGFR2, AKT, MEK and ERK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CAL27 xenograft model in male BALB/c nude mice (four-week-old)[1]
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Dosage:30 and 60 mg/kg
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Administration:i.g. ; once daily for 21 days
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Result:Suppressed tumor growth in a dose-dependent manner.
Achieved a tumor growth inhibition rate of 47.7% at the dose of 60 mg/kg.
Induced tumor necrosis in a dose-dependent manner.
No significant body weight changes.
No notable abnormalities in heart, liver, or kidney.
Chemical Information
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Molecular Weight 585.68
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Formula C30H31N7O4S
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SMILES
CN1CCN(CC1)S(=O)(C2=CC=C(C=C2)C3=NC(C(NC4=CC=C(C=C4)CC(NC5=CC=CC=C5)=O)=O)=C(N=C3)N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-3β/VEGFR2-IN-1 Related Classifications
HY-184741 Related Classifications
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