[CAS NO. 212141-54-3] Vatalanib
PRODUCTS SPECIFICATIONS [212141-54-3]
DESCRIPTION [212141-54-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 346.81 |
| Molecular Formula | C20H15ClN4 |
| SMILES | ClC1=CC=C(C=C1)NC2=NN=C(CC3=CC=NC=C3)C4=C2C=CC=C4 |
12 Publications Citing Use of MCE
- [1]Bioact Mater. 2 January 2022.
- [2]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
- [3]J Pharm Anal. 2023 Sep 11.
- [4]Br J Pharmacol. 2019 Sep;176(17):3143-3160.
- [5]Oncol Rep. 2016 Mar;35(3):1297-308.
- [6]J Microbiol Biotechnol. 2015 Aug;25(8):1227-33.
- [7]Drug Metab Pharmacokinet. 2017 Jun;32(3):179-188.
- [8]Ulm University. 2023 Mar 21.
- [9]Oxid Med Cell Longev. 18 Jul 2022.
- [10]Evid-Based Compl Alt. 2021 Apr 27.
- [11]Patent. US20170349880A1.
- [12]Kitazato Graduate School of Pharmaceutical Sciences. Kitasato University. 2017.
Summary
Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC 50 of 37 nM.
IC50 & Target
|
VEGFR2 37 nM (IC 50 ) |
In Vitro
Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC 50 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 IC 50 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] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00072475 | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) |
Leukemia|Myelodysplastic Syndromes|Myelodysplastic+Myeloproliferative Neoplasms
|
December 2003 | Phase 2 |
| NCT00281125 | Nevada Cancer Institute |
Non-Small Cell Lung Cancer and Pleural Mesothelioma
|
January 2006 | Phase 1|Phase 2 |
| NCT00088231 | M.D. Anderson Cancer Center|Novartis |
Acute Myelogenous Leukemia|Agnogenic Myeloid Metaplasia|Chronic Myelogenous Leukemia
|
July 2004 | Phase 1|Phase 2 |
| NCT00348790 | Northwestern University|Novartis |
Brain and Central Nervous System Tumors|Sarcoma
|
May 2006 | Phase 2 |
| NCT00731861 | Indiana University School of Medicine|Novartis|Indiana University |
Neoplasm Metastasis|Carcinoma
|
May 2005 | Phase 1 |
| 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 |
| 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 |
| NCT00160043 | Bayer |
Non Small Cell Lung Cancer
|
March 2005 | Phase 2 |
| NCT00134355 | University of Michigan Rogel Cancer Center|Novartis |
Prostate Cancer
|
July 2005 | 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 Cell Cancer|Thyroid Gland Medullary Carcinoma|Unspecified Adult Solid Tumor, Protocol Specific
|
December 2004 | Phase 1 |
| NCT00511043 | David Rizzieri, MD|Novartis Pharmaceuticals|Duke University |
Lymphoma, Large-Cell, Diffuse
|
November 2005 | Phase 2 |
| NCT00056446 | Novartis Pharmaceuticals|Bayer|Novartis |
Colorectal Neoplasms|Colonic Neoplasms|Rectal Neoplasms
|
January 2003 | Phase 3 |
| NCT00216047 | Hoosier Cancer Research Network|Novartis Pharmaceuticals|Walther Cancer Institute |
Breast Cancer
|
January 2005 | Phase 1|Phase 2 |
| NCT00390000 | Mayo Clinic|National Cancer Institute (NCI) |
Unspecified Adult Solid Tumor, Protocol Specific
|
January 25, 2007 | Phase 1 |
| NCT00227773 | Eastern Cooperative Oncology Group|National Cancer Institute (NCI) |
Gastrointestinal Carcinoid Tumor|Islet Cell Carcinoma
|
Phase 2 | |
| NCT00387933 | Duke University|National Cancer Institute (NCI) |
Brain and Central Nervous System Tumors
|
July 2005 | Phase 1 |
| NCT00138632 | Novartis |
Wet Age-Related Macular Degeneration
|
September 2005 | Phase 1|Phase 2 |
| NCT00056459 | Novartis|Bayer |
Colorectal Neoplasms|Colonic Neoplasms|Rectal Neoplasms
|
February 2003 | Phase 3 |
| NCT00303732 | Daniel George, MD|Novartis|Duke University |
Kidney Cancer|Unspecified Adult Solid Tumor, Protocol Specific
|
December 2004 | Phase 1 |
| NCT00293371 | University of California, San Francisco|National Cancer Institute (NCI) |
Prostate Cancer
|
February 2005 | Phase 1|Phase 2 |
| NCT00185588 | George Albert Fisher|Novartis|Stanford University |
Pancreatic Cancer
|
October 2004 | Phase 1|Phase 2 |
| NCT00590343 | Louisiana State University Health Sciences Center in New Orleans|Novartis |
Metastatic Neuroendocrine Tumors
|
November 2004 | Phase 2 |
| NCT00171587 | Novartis|Bayer |
Tumors|Neoplasm Metastasis
|
May 2002 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 180.21 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8834 mL | 14.4171 mL | 28.8342 mL |
| 5 mM | 0.5767 mL | 2.8834 mL | 5.7668 mL |
| 10 mM | 0.2883 mL | 1.4417 mL | 2.8834 mL |
References
- [1] Wood JM, et al. 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. Cancer Res. 2000, 60(8
- [2] Murakami M, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011, 18(2), 589-596.
- [3] Wan J, et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308.