2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. ZK-261991

ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.

For research use only. We do not sell to patients.

ZK-261991 Chemical Structure

ZK-261991 Chemical Structure

CAS No. : 886563-25-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

ZK-261991 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

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.

IC50 & Target[1]

VEGFR2

5 nM (IC50)

In Vitro

ZK-261991 inhibits cellular receptor autophosphorylation in KDR-PAECs with an IC50 of 2 nM. ZK991 inhibits VEGFR-3 autophosphorylation concentration dependently with an IC50 of 20 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZK-261991 Related Antibodies
In Vivo

ZK991 results in a significantly reduced recruitment of CD11b+ and LYVE-1+ cells into the murine cornea. ZK991 significantly improves the graft survival rate after corneal transplantation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

443.50

Formula

C24H25N7O2
CAS No.
SMILES

O=C(NC1=CC2=NN(C)C=C2C=C1)C3=CC=CC=C3NCC4=CC(NC(N(C)C)=O)=NC=C4
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
Cell Assay
[1]

HLMVECs are cultured in EGM 2-MV medium. For the cytotoxicity assay, cells are seeded in 96-well plates in EGM 2-MV medium at a density of 5×103 cells/well. Medium is changed every second day, and cells are cultured until reaching confluence. Then the medium is replaced with serum-free medium containing a tyrosine kinase inhibitor (PTK/ZK or ZK991; concentration 20 nM) and left overnight. Control cells receive the substance vehicle. The next day, cytotoxicity assay (WST-1 based) is performed according to the manufacturer's instructions. Colorimetric analysis is performed with an ELISA reader. Subsequent statistical analysis is performed, and graphs are drawn. The number of wells per group is as follows: PTK/ZK control group, n = 30; PTK/ZK 20 nM, n = 30; ZK991 control group, n = 30; ZK991 20 nM, n = 30.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Before corneal neovascularization, each animal is deeply anesthetized. Three 11-0 nylon sutures are placed intrastromally with two stromal incursions extending over 120°C of corneal circumference each. The outer point of suture placement is chosen near the limbus, and the inner suture point is chosen near the corneal center equidistant from the limbus to obtain standardized angiogenic responses. Sutures are left in place for 14 days. The first treatment group receive the tyrosine kinase inhibitor PTK/ZK (75 mg/kg, orally, twice daily), the second treatment group receive the tyrosine kinase inhibitor ZK991 (50 mg/kg, orally, twice daily), and control mice receive equal amounts of the substance vehicle. After 2 weeks, mice are killed and corneas are prepared. The corneal neovascularization assay includes 22 mice in the control group, 11 mice in the PTK/ZK treatment group, and 11 mice in the ZK991 treatment group.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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.

ZK-261991 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:

ZK-261991886563-25-3ZK261991ZK 261991VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ZK-261991
Cat. No.:
HY-15333
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

Request for HNMR Report

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