Vatalanib (PTK787) 2HCl

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.

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Vatalanib (PTK787) 2HCl Chemical Structure

Vatalanib (PTK787) 2HCl Chemical Structure
Molecular Weight: 419.73

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Customer Reviews(2)

Quality Control & MSDS

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Product Information

  • Inhibition Profile
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Product Description

Biological Activity

Description Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.
Targets VEGFR2/KDR Flt-1 c-Kit
IC50 37 nM 77 nM 730 nM [1]
In vitro Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Furthermore, 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

VEGF Receptor Tyrosine Kinase Assays The in vitro kinase assays are performed in 96-well plates as a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-Sepharose. γ-[33P]ATP is used as the phosphate donor, and poly-(Glu:Tyr 4:1) peptide is used as the acceptor. Recombinant GST-fusion proteins are diluted in 20 mM Tris·HCl (pH 7.5) containing 1–3 mM MnCl2, 3–10 mM MgCl2, 0.25 mg/mL polyethylene glycol 20000, and 1 mM DTT, according to their specific activity. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1–3 mM MnCl2, 3–10 mM MgCl2, 3–8 μg/mL poly-(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT, and 0.2 μCi[γ-33P]ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 minutes at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA. Using a 96-well filter system, half the volume (20 μL) is transferred onto a Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively in 0.5% H3PO4 and then soaked in ethanol. After drying, Microscint cocktail is added, and scintillation counting is performed. IC50s for PTK787/ZK 222584 or SU5416 in these as well as all assays described below are calculated by linear regression analysis of the percentage inhibition.

Cell Assay: [1]

Cell lines HUVECs
Concentrations 0-10 μM
Incubation Time 48 hours
Method 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 is used. Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin and then incubated at 37 °C and 5% CO2 in growth medium. After 24 hours, 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 hours of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 hours before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3′5,5′-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm.

Animal Study: [1]

Animal Models A431 epithelial carcinoma, Ls174T colon carcinoma, HT-29 colon carcinoma, PC-3 prostate carcinoma, DU145 prostate carcinoma, and CWR-22 prostate carcinoma cells are injected s.c. into the nude mice.
Dosages 25-100 mg/kg
Administration Administered via p.o.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
1

References

Chemical Information

Download Vatalanib (PTK787) 2HCl SDF
Molecular Weight (MW) 419.73
Formula

C20H15ClN4.2HCl

CAS No. 212141-51-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 85 mg/mL (202 mM)
Water 10 mg/mL (23 mM)
Ethanol 6 mg/mL (14 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine dihydrochloride

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.41973 4.1973 8.3946 12.5919

Research Area

Customer Reviews (2)


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Rating
Source Cell Res 2011 21, 1080-1087. Vatalanib (PTK787) 2HCl purchased from Selleck
Method Microangiography
Cell Lines embryos
Concentrations 30 μM
Incubation Time
Results Both of these inhibitors (PTK787 or ZM323881), when individually combined with Dasatinib or U0126, induced a reduction of vessel lumen size. However, they did not lead to this phenotype when added alone.

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Rating
Source Circ Res 2011 108, 1190-1198. Vatalanib (PTK787) 2HCl purchased from Selleck
Method Immunofluorescence
Cell Lines HUVECs
Concentrations 10 nmol/L
Incubation Time
Results The multikinase inhibitors sorafenib and vatalanib potently suppressed VEGF-evoked Ca2+ rises (Figure a). HUVECs were transfected with eYFP-tagged STIM1 which showed the expected 14 microtubule-like localization pattern (Figure b). VEGF caused marked clustering of eYFP-STIM1 (Figure c). Additional experiments were carried out where endogenous STIM1 was knocked down by RNA interference (Figure d). STIM1 siRNA suppressed VEGF-evoked Ca2+ signals (Figure d).

Product Citations (7)

Tech Support & FAQs

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