Vatalanib (PTK787) 2HCl
Catalog No.S1101 Synonyms: ZK 222584 (cpg-79787) 2HCl
Molecular Weight(MW): 419.73
Vatalanib (PTK787) 2HCl is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.
Cited by 19 Publications
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|Description||Vatalanib (PTK787) 2HCl is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.|
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.  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. 
|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. |
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.
|In vitro||DMSO||85 mg/mL (202.51 mM)|
|Water||10 mg/mL (23.82 mM)|
|Ethanol||6 mg/mL (14.29 mM)|
* 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.
|Synonyms||ZK 222584 (cpg-79787) 2HCl|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00348790||Completed||Drug: vatalanib||Brain and Central Nervous System Tumors|Sarcoma||Northwestern University|Novartis||May 2006||Phase 2|
|NCT00358163||Unknown status||Drug: PTK787/ZK 222584|Drug: paclitaxel||Metastatic Non-hematologic Malignancies||Massachusetts General Hospital|Novartis Pharmaceuticals|Beth Israel Deaconess Medical Center|Brigham and Women''s Hospital|Dana-Farber Cancer Institute||April 2006||Phase 1|
|NCT00263198||Terminated||Drug: PTK787/ZK222584|Drug: Letrozole||Breast Neoplasms||Washington University School of Medicine|Novartis||March 2006||Phase 2|
|NCT00281125||Terminated||Drug: PTK787 and Pemetrexed with or without Cisplatin||Non-Small Cell Lung Cancer and Pleural Mesothelioma||Nevada Cancer Institute||January 2006||Phase 1|Phase 2|
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