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

Vatalanib  (Synonyms: PTK787; ZK-222584; CGP-79787)

Cat. No.: HY-10203 Purity: 99.86%
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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 Chemical Structure

Vatalanib Chemical Structure

CAS No. : 212141-54-3

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Based on 12 publication(s) in Google Scholar

Other Forms of Vatalanib:

Vatalanib 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

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].

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

Vatalanib Related Antibodies
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].

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

346.81

Formula

C20H15ClN4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (180.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8834 mL 14.4171 mL 28.8342 mL 72.0856 mL
5 mM 0.5767 mL 2.8834 mL 5.7668 mL 14.4171 mL
10 mM 0.2883 mL 1.4417 mL 2.8834 mL 7.2086 mL
15 mM 0.1922 mL 0.9611 mL 1.9223 mL 4.8057 mL
20 mM 0.1442 mL 0.7209 mL 1.4417 mL 3.6043 mL
25 mM 0.1153 mL 0.5767 mL 1.1534 mL 2.8834 mL
30 mM 0.0961 mL 0.4806 mL 0.9611 mL 2.4029 mL
40 mM 0.0721 mL 0.3604 mL 0.7209 mL 1.8021 mL
50 mM 0.0577 mL 0.2883 mL 0.5767 mL 1.4417 mL
60 mM 0.0481 mL 0.2403 mL 0.4806 mL 1.2014 mL
80 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9011 mL
100 mM 0.0288 mL 0.1442 mL 0.2883 mL 0.7209 mL
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Vatalanib Related Classifications

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:

Vatalanib212141-54-3PTK787 ZK-222584 CGP-79787PTK 787PTK-787ZK222584ZK 222584ZK-222584CGP79787CGP 79787CGP-79787VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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