HIF-1 inhibitor-5
HIF-1 inhibitor-5 (Compound 16e) is a potent HIF-1 inhibitor with an IC50 of 2.38 μM. HIF-1 inhibitor-5 possesses anti-angiogenic potential.
For research use only. We do not sell to patients.
- Formula: C28H35NO5
- Molecular Weight:465.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 2.38 μM (HIF-1)[1]
HIF-1 inhibitor-5 (Compound 16e; 0-4 μM; 24 h) suppresses A549 cell migration and invasion[1].
HIF-1 inhibitor-5 (0-8 μM; 12 h) blocks VEGF-induced tube formation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and HUVEC cells
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Concentration:0-128 μM
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Incubation Time:48 h
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Result:Showed cytotoxic effects with IC50s of 8.883 μM and 19.599 μM for A549 and HUVEC cells, respectively.
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Cell Line:A549 cell
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Concentration:0, 2 and 4 μM
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Incubation Time:24 h
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Result:The number of migrated A549 cells decreased significantly.
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Cell Line:A549 cell
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Concentration:0, 2 and 4 μM
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Incubation Time:24 h
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Result:Inhibited cell invasion at a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/bl6 female mice, VEGF-induced angiogenesis model[1]
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Dosage:1.25, 5 and 20 μM
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Administration:0.5 mL of matrix glue subcutaneously injected near the midline of abdomen
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Result:Decreased the number of blood vessels.
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Animal Model:SD rats
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Dosage:20 mg/kg
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Administration:Intravenous administration (Pharmacokinetic Study)
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Result:Pharmacokinetic parameters of HIF-1 inhibitor-5 (Compound 16e) in rats after intravenous administrationa[1]
Parameter iv (20 mg/kg) (n = 2) Tmax (h) 0.033 Cmax (μmol/L) 7.06 T1/2 (h) 1.64 CL (mL/h) 2368.50 VZ (L) 5.59 AUC0-t (μmol•h/L) 5.27 AUC0-∞ (μmol•h/L) 8.88
aAfter administration, blood samples were collected at different time (0, 0.083, 0.17, 0.5, 1, 2, 4, 6 h). The combination of compounds in a ratio of 8% ethanol absolute, 4% Tween-80 and 88% normal saline was chosen for the intravenous injection formulation.
Chemical Information
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Molecular Weight 465.58
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Formula C28H35NO5
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SMILES
O=C(C1=C(C2=C(OC(C)(C=C2)C)C=C1)O)/C=C/C3=CC(C(C=C3)OC)OCCCN4CCCC4
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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)