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Vatalanib dihydrochloride

Cat. No. M1882

All AbMole products are for research use only, cannot be used for human consumption.

Vatalanib dihydrochloride Structure
Synonym:

PTK787; ZK-222584 dihydrochloride

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 30  USD30 In stock
10mg USD 45  USD45 In stock
50mg USD 70  USD70 In stock
100mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

Vandetanib Dihydrochloride (PTK787) is an orally VEGF receptors inhibitor that inhibits angiogenesis (IC50 = 37 nM and 77 nM for KDR and Flt-1 respectively). The vascular endothelial growth factor (VEGF) is a central mediator of tumor-induced angiogenesis. Vandetanib (PTK787) was hypothesized that dual inhibition of VEGF signaling by inhibition of VEGF production and VEGF receptor signaling leads to synergistic anti-tumor effects. Vatalanib abolished endothelial cell tube formation, whereas inhibition of tube formation by everolimus was incomplete.

In vivo, the combination of vatalanib with everolimus was superior to single agent treatments and reduced tumor size by about 50% relative to everolimus monotherapy (p < 0.005). Furthermore, Vatalanib dihydrochloride shows significant inhibition of hepatocellular carcinoma cells growth and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines HUVECs
Preparation method Endothelial Cell Proliferation Assays.
As a test of the ability of PTK787/ZK 222584 to inhibit a functional response to VEGF, an endothelial cell proliferation assay, based on BrdUrd incorporation was used (Biotrak Cell Proliferation System V.2, Amersham, England). Subconfluent HUVECs were seeded at a density of 5 3 103 cells/well into 96-well plates coated with 1.5% gelatin and then incubated at 37°C and 5% CO2 in growth medium. After 24 h, growth medium was 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 were also included. After 24 h of incubation, BrdUrd labeling solution was added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody was then detected using 3,395,59-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm.
Concentrations 0~1 μM
Incubation time 24 h
Animal Experiment
Animal models Nude Mouse Human Tumor Xenograft Model
Formulation distilled water
Dosages 25 to 100 mg/kg once or twice dail
Administration p.o.
Chemical Information
Molecular Weight 419.73
Formula C20H15ClN4.2HCl
CAS Number 212141-51-0
Solubility (25°C) DMSO 48 mg/mL
Water 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Jaeger-Lansky A, et al. Cancer Biol Ther. Effects of vatalanib on tumor growth can be potentiated by mTOR blockade in vivo.

[2] Wood JM, et al. Cancer Res. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.

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  Catalog
Abmole Inhibitor Catalog




Keywords: Vatalanib dihydrochloride, PTK787; ZK-222584 dihydrochloride supplier, VEGFR/PDGFR, inhibitors, activators

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