EYE1090
EYE1090 is an orally active VEGFR2 inhibitor with an IC50 of 3 nM. EYE1090 inhibits angiogenesis, endothelial migration, VEGFR2-induced retinal leakage, and reduces choroidal neovascularization lesion size in mice. EYE1090 can be used for the research of age-related macular degeneration, diabetic retinopathy, choroidal neovascularization.
For research use only. We do not sell to patients.
- CAS No.: 3037217-70-9
- Formula: C22H26ClN7O2
- Molecular Weight:455.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All VEGFR Isoforms
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Biological Activity
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VEGFR-2 |
EYE1090 inhibits purified VEGFR2 kinase with an IC50 of 13 nM in the dark, and illumination enhances this potency to an IC50 of 3 nM[1].
EYE1090 (0.1-100 μM; 24 h) reduces NIH/3T3 fibroblast viability in a dose-dependent manner[1].
EYE1090 (50 min pre-incubation; 10 min light exposure; 4 h VEGF stimulation) inhibits VEGF-induced VEGFR2 signaling in VEGFR2/NFAT Reporter-HEK293 cells with an IC50 of 19.06 nM in the dark under cold white LED conditions, 21.75 nM under red LED conditions, and 33.37 nM under green LED conditions; illumination with cold white or green LED significantly enhances potency, while red LED has no effect[1].
EYE1090 (1-100 nM; 1 h pre-incubation; 10 min light exposure; 10 min VEGF stimulation) does not significantly inhibit VEGF-induced VEGFR2 phosphorylation at Y951 or Y1175 in VEGFR2/NFAT Reporter-HEK293 cells in the dark, but light exposure triggers potent inhibition of phosphorylation at these sites[1].
EYE1090 (0.1 nM-10 μM; 10 min pre-incubation; 10 min light exposure; 12 h incubation) inhibits HRMEC tubulogenesis with an IC50 of 410 nM in the dark, and light exposure enhances this potency to an IC50 of 133 nM, eliminating the potency gap with sunitinib[1].
EYE1090 (0.001-10 μM; 10 min pre-incubation; 10 min light exposure; 6 h migration incubation) inhibits HRMEC migration with an IC50 of 1012 nM in the dark, and light exposure enhances this potency to an IC50 of 474 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NIH/3T3 fibroblasts
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Concentration:0.1; 1; 10; 50; 75; 100 μM
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Incubation Time:24 h
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Result:Reduced NIH/3T3 cell viability in a dose-dependent manner.
Was significantly less toxic than its parental compound sunitinib at concentrations above 75 μM (p<0.05).
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Cell Line:VEGFR2/NFAT Reporter-HEK293 recombinant cell line
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Concentration:1; 10; 50; 100 nM
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Incubation Time:1 h pre-incubation; 10 min light exposure; 10 min VEGF stimulation
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Result:Did not substantially inhibit VEGF-induced phosphorylation of VEGFR2 at Y951 or Y1175 in the dark, even at 100 nM.
Significantly suppressed VEGF-induced phosphorylation of VEGFR2 at Y951 or Y1175 with light exposure.
Left total VEGFR2 and β-actin levels unchanged, confirming no receptor degradation or loading differences.
EYE1090 (1 mg/kg; i.g.; daily; 3 days) significantly reduces VEGF-induced retinal vascular leakage in Long Evans rats[1].
EYE1090 (1 mg/kg; i.g.; daily; 3 days) significantly reduces choroidal neovascularization (CNV) lesion area in mice[1].
EYE1090 (40 mg/kg; i.g.; single dose) does not cause hepatotoxicity in mice under normal or dim red light conditions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cJRj mice (male, 8 weeks old)[1]
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Dosage:40 mg/kg
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Administration:i.g.; single dose
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Result:Reduced mean serum concentrations by more than 50% in white light-exposed group compared to dark-treated controls.
Increased significantly in the dark condition.
Showed no significant increase in the light-exposed group.
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Animal Model:Long Evans rats (male, 200-250 g) intravitreally injected with VEGF (50 ng/eye) on day3[1]
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Dosage:1 mg/kg
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Administration:i.g.; daily; 3 days
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Result:Reduced VEGF-induced retinal vascular permeability significantly, with permeability values in VEGF-injected eyes significantly lower than those in VEGF-only control eyes.
Showed permeability values not significantly different from control eyes without VEGF injection.
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Animal Model:Adlut C57BL/6JRj mice (9 weeks old) with choroidal neovascularization (CNV)[1]
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Dosage:1 mg/kg
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Administration:i.g.; daily; 3 days
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Result:Reduced CNV lesion area highly significantly compared to vehicle controls by day 5.
Decreased lesion area through day 7, remaining significantly lower than vehicle controls.
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Animal Model:BALB/cJRj (male and female, 6-10 weeks old)[1]
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Dosage:40 mg/kg
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Administration:i.g.; single dose
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Result:Showed intact liver architecture, normal glycogen storage, and no evidence of necrosis, cellular stress, fibrosis, or abnormal collagen deposition under either normal light/dark cycles or continuous dim red light conditions.
Chemical Information
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CAS No. 3037217-70-9
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Molecular Weight 455.94
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Formula C22H26ClN7O2
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SMILES
CCN(CC)CCNC(C1=C(C)NC(/C=C2C(NC3=CC(Cl)=C(N=[N+]=[N-])C=C3\2)=O)=C1C)=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)