1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Vatalanib free base

Vatalanib free base (Synonyms: PTK787 free base; PTK/ZK free base; CGP-79787 free base; ZK-222584 free base)

Cat. No.: HY-10203
Handling Instructions

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.

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

Vatalanib free base Chemical Structure

Vatalanib free base Chemical Structure

CAS No. : 212141-54-3

Size Price Stock
5 mg USD 60 Get quote
10 mg USD 84 Get quote
50 mg USD 216 Get quote

* Please select Quantity before adding items.

Other In-stock Forms of Vatalanib free base:

Other Forms of Vatalanib free base:

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.

IC50 & Target[1]

VEGFR2

37 nM (IC50)

In Vitro

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors[1]. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2[2].

In Vivo

Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes[1].

Clinical Trial
Molecular Weight

346.81

Formula

C₂₀H₁₅ClN₄

CAS No.

212141-54-3

SMILES

ClC1=CC=C(C=C1)NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (360.43 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8834 mL 14.4171 mL 28.8342 mL
5 mM 0.5767 mL 2.8834 mL 5.7668 mL
10 mM 0.2883 mL 1.4417 mL 2.8834 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Each GST-fused kinase is incubated under optimized buffer conditions. ATP in a total volume of 30 μL in the presence or absence of a test substance (Vatalanib) for 10 min at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA[1].

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

Cell Assay
[1]

Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin. After 24 h, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of Vatalanib. As a control, wells without growth factor are also included. After 24 h of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3' 5,5'-tetramethylbenzidine substrate[1].

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

Animal Administration
[1]

A porous Teflon chamber (volume, 0.5 mL) is filled with 0.8% w/v agar containing heparin (20 units/mL) with or without growth factor (3 μg/mL human VEGF, 2 μg/mL human PDGF) is implanted s.c. on the dorsal flank of C57/C6 mice. The mice are treated with Vatalanib (12.5, 25 or 50 mg/kg dihydrochloride p.o. once daily) or vehicle (water) starting 1 day before implantation of the chamber and continuing for 5 days after. At the end of treatment, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is carefully removed and weighed, and the blood content is assessed by measuring the hemoglobin content of the tissue[1].

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.
  • 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

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Vatalanib free base
Cat. No.:
HY-10203
Quantity: