Vatalanib succinate

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Cat.No. 5680 - Vatalanib succinate | C20H15ClN4.C4H6O4 | CAS No. 212142-18-2
Description: Potent VEGFR inhibitor; also aromatase inhibitor
Alternative Names: CGP 79787D, PTK787/ZK222584
Chemical Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine succinate
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Potent VEGFR inhibitor (IC50 values are 37 and 77 nM for VEGFR-2 and -1, respectively). Inhibits proliferation, migration and survival of HUVECs in vitro and inhibits growth, vascularization and metastasis of tumors expressing VEGFR in mouse models. Also inhibits PDGFR-β, c-Kit and c-Fms. Potent aromatase inhibitor (IC50 = 50 nM). Orally available.

Compound Libraries

Vatalanib succinate is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 464.9
Formula C20H15ClN4.C4H6O4
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 212142-18-2
PubChem ID 151193
InChI Key LLDWLPRYLVPDTG-UHFFFAOYSA-N
Smiles ClC(C=C1)=CC=C1NC2=NN=C(CC3=CC=NC=C3)C4=CC=CC=C42.OC(CCC(O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.49 100

Preparing Stock Solutions

The following data is based on the product molecular weight 464.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.15 mL 10.76 mL 21.51 mL
5 mM 0.43 mL 2.15 mL 4.3 mL
10 mM 0.22 mL 1.08 mL 2.15 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Banerjee et al (2009) The vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 inhibits aromatase. Cancer Res. 69 4716 PMID: 19435899

Wood et al (2000) 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. 60 2178 PMID: 0786682

Bold et al (2000) New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J.Med.Chem. 43 2310 PMID: 10956229


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View all VEGFR Inhibitors

Keywords: Vatalanib succinate, supplier, CGP79787D, PTK787, ZK222584, aromatase, inhibitors, inhibits, vascular, endothelial, growth, factor, receptors, tyrosine, kinases, cancer, anticancer, VEGFR, angiogenesis, metastasis, CGP, 79787D, PTK787/ZK222584, VEGFR, Cytochrome, P450, VEGFR, Tocris Bioscience

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Vatalanib succinate

VEGF

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.