2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. 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.

EYE1090

EYE1090 Chemical Structure

CAS No. : 3037217-70-9

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

EYE1090 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

VEGFR-2

 

In Vitro

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.

EYE1090 Related Antibodies

Cell Viability Assay[1]

Cell Line: NIH/3T3 fibroblasts
Concentration: 0.1; 1; 10; 50; 75; 100 μM
Incubation Time: 24 h
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).

Western Blot Analysis[1]

Cell Line: VEGFR2/NFAT Reporter-HEK293 recombinant cell line
Concentration: 1; 10; 50; 100 nM
Incubation Time: 1 h pre-incubation; 10 min light exposure; 10 min VEGF stimulation
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.
In Vivo

EYE1090 (40 mg/kg; i.g.; single dose) has light exposure significantly reduce its systemic serum concentrations in mice[1].
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.

Animal Model: BALB/cJRj mice (male, 8 weeks old)[1]
Dosage: 40 mg/kg
Administration: i.g.; single dose
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.
Animal Model: Long Evans rats (male, 200-250 g) intravitreally injected with VEGF (50 ng/eye) on day3[1]
Dosage: 1 mg/kg
Administration: i.g.; daily; 3 days
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.
Animal Model: Adlut C57BL/6JRj mice (9 weeks old) with choroidal neovascularization (CNV)[1]
Dosage: 1 mg/kg
Administration: i.g.; daily; 3 days
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.
Animal Model: BALB/cJRj (male and female, 6-10 weeks old)[1]
Dosage: 40 mg/kg
Administration: i.g.; single dose
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.
Molecular Weight

455.94

Formula

C22H26ClN7O2
CAS No.
SMILES

CCN(CC)CCNC(C1=C(C)NC(/C=C2C(NC3=CC(Cl)=C(N=[N+]=[N-])C=C3\2)=O)=C1C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

EYE1090 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EYE10903037217-70-9EYE 1090EYE-1090VEGFRVascular endothelial growth factor receptordiabetic retinopathychoroidal neovascularizationVEGFR2HRMECendothelial migrationage-related macular degenerationVEGF-induced retinal leakageVEGFR2/NFAT Reporter-HEK293 cellsNIH/3T3 fibroblastangiogenesisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EYE1090
Cat. No.:
HY-184141
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.