1. Protein Tyrosine Kinase/RTK
  2. VEGFR

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

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 Chemical Structure

Vatalanib Chemical Structure

CAS No. : 212141-51-0

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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
NCT Number Sponsor Condition Start Date Phase
NCT00511043 David Rizzieri, MD|Novartis Pharmaceuticals|Duke University Lymphoma, Large-Cell, Diffuse November 2005 Phase 2
NCT00268918 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Massachusetts General Hospital Ovarian Cancer|Endometrial Cancer|Cervical Cancer|Fallopian Tube Cancer|Peritoneal Cancer|Breast Cancer September 2005 Phase 1
NCT00731861 Indiana University School of Medicine|Novartis|Indiana University Neoplasm Metastasis|Carcinoma May 2005 Phase 1
NCT00134355 University of Michigan Cancer Center|Novartis Prostate Cancer July 2005 Phase 2
NCT00117299 Helsinki University|Bayer Sarcoma September 2004 Phase 2
NCT00358163 Massachusetts General Hospital|Novartis Pharmaceuticals|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|Dana-Farber Cancer Institute Metastatic Non-hematologic Malignancies April 2006 Phase 1
NCT00226005 Pancreatic Cancer Research Team Neoplasm December 2005 Phase 2
NCT00053885 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Malignant Mesothelioma July 2003 Phase 2
NCT00611793 SCRI Development Innovations, LLC|Novartis Refractory Malignancy|Advanced Malignancies October 2004 Phase 1
NCT00216047 Hoosier Cancer Research Network|Novartis Pharmaceuticals|Walther Cancer Institute Breast Cancer January 2005 Phase 1|Phase 2
NCT00052013 Novartis Pharmaceuticals|Novartis Von Hippel-Lindau Disease|CNS Hemangioblastoma|Retinal Hemangioblastoma February 2003 Phase 2
NCT00281125 Nevada Cancer Institute Non-Small Cell Lung Cancer and Pleural Mesothelioma January 2006 Phase 1|Phase 2
NCT00385853 Massachusetts General Hospital|Dana-Farber Cancer Institute|Novartis Glioblastoma September 2006 Phase 1
NCT00138632 Novartis Wet Age-Related Macular Degeneration September 2005 Phase 1|Phase 2
NCT00263198 Washington University School of Medicine|Novartis Breast Neoplasms March 2006 Phase 2
NCT00303732 Daniel George, MD|Novartis|Duke University Kidney Cancer|Unspecified Adult Solid Tumor, Protocol Specific December 2004 Phase 1
NCT00627198 University of Iowa|Novartis Pharmaceuticals Neuroendocrine Tumors December 2006 Phase 2
NCT00240162 Washington University School of Medicine Multiple Myeloma September 2005 Phase 2
NCT00171587 Novartis|Bayer Tumors|Neoplasm Metastasis May 2002 Phase 1|Phase 2
NCT00165347 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Novartis Multiple Myeloma December 2003 Phase 2
NCT00160043 Bayer Non Small Cell Lung Cancer March 2005 Phase 2
NCT00615160 University of Schleswig-Holstein Melanoma December 2006 Phase 1|Phase 2
NCT00348790 Northwestern University|Novartis Brain and Central Nervous System Tumors|Sarcoma May 2006 Phase 2
NCT00072475 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Neoplasms December 2003 Phase 2
NCT00590343 Louisiana State University Health Sciences Center in New Orleans|Novartis Metastatic Neuroendocrine Tumors November 2004 Phase 2
NCT00088231 M.D. Anderson Cancer Center|Novartis Acute Myelogenous Leukemia|Agnogenic Myeloid Metaplasia|Chronic Myelogenous Leukemia July 2004 Phase 1|Phase 2
NCT00387933 Duke University|National Cancer Institute (NCI) Brain and Central Nervous System Tumors July 2005 Phase 1
NCT00056459 Novartis|Bayer Colorectal Neoplasms|Colonic Neoplasms|Rectal Neoplasms February 2003 Phase 3
NCT00056446 Novartis Pharmaceuticals|Bayer|Novartis Colorectal Neoplasms|Colonic Neoplasms|Rectal Neoplasms January 2003 Phase 3
NCT00185588 George Albert Fisher|Novartis|Stanford University Pancreatic Cancer October 2004 Phase 1|Phase 2
NCT00563823 Cambridge University Hospitals NHS Foundation Trust|National Cancer Institute (NCI) Melanoma (Skin) February 2006 Phase 2
NCT00128700 European Organisation for Research and Treatment of Cancer - EORTC Brain and Central Nervous System Tumors June 2005 Phase 1|Phase 2
NCT00655655 Mayo Clinic|National Cancer Institute (NCI) Gastrinoma|Glucagonoma|Insulinoma|Metastatic Gastrointestinal Carcinoid Tumor|Metastatic Pheochromocytoma|Pancreatic Polypeptide Tumor|Recurrent Gastrointestinal Carcinoid Tumor|Recurrent Islet Cell Carcinoma|Recurrent Melanoma|Recurrent Neuroendocrine Carcinoma of the Skin|Recurrent Non-small Cell Lung Cancer|Recurrent Pheochromocytoma|Recurrent Renal Cell Cancer|Somatostatinoma|Stage III Neuroendocrine Carcinoma of the Skin|Stage IV Melanoma|Stage IV Non-small Cell Lung Cancer|Stage IV Renal C December 2004 Phase 1
NCT00293371 University of California, San Francisco|National Cancer Institute (NCI) Prostate Cancer February 2005 Phase 1|Phase 2
NCT00227773 Eastern Cooperative Oncology Group|National Cancer Institute (NCI) Gastrointestinal Carcinoid Tumor|Islet Cell Carcinoma Phase 2
NCT00390000 Mayo Clinic|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific January 2007 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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
M.Wt

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

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

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Vatalanib
Cat. No.:
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