1. Protein Tyrosine Kinase/RTK
  2. VEGFR

Vatalanib dihydrochloride (Synonyms: PTK787 dihydrochloride; PTK/ZK dihydrochloride; CGP-79787D dihydrochloride; CGP-79787 dihydrochloride; ZK-222584 dihydrochloride)

Cat. No.: HY-12018 Purity: 99.86%
Data Sheet SDS 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 dihydrochloride Chemical Structure

Vatalanib dihydrochloride Chemical Structure

CAS No. : 212141-51-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $70 In-stock
100 mg $110 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of Vatalanib dihydrochloride:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 37 nM (VEGFR2/KDR)[1]

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
View MoreCollapse
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.3825 mL 11.9124 mL 23.8248 mL
5 mM 0.4765 mL 2.3825 mL 4.7650 mL
10 mM 0.2382 mL 1.1912 mL 2.3825 mL
Please refer to the solubility information to select the appropriate solvent.
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 for 10 min at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA. Us 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 PTK787/ZK 222584. 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 PTK787/ZK 222584 (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
Molecular Weight

419.73

Formula

C₂₀H₁₇Cl₃N₄

CAS No.

212141-51-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Vatalanib (PTK/ZK) is dissolved in polyethyleneglycol 400[3].

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

References

Purity: 99.86%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Vatalanib dihydrochloride
Cat. No.:
HY-12018
Quantity: