Vatalanib succinate

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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 (2)
Reviews
Literature (1)
Pathways (1)

Biological Activity for Vatalanib succinate

Vatalanib succinate is a 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.

Technical Data for Vatalanib succinate

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Vatalanib succinate

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

Preparing Stock Solutions for Vatalanib succinate

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

Select a batch to recalculate based on the batch molecular weight:
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 for Vatalanib succinate

References for Vatalanib succinate

References are publications that support the biological activity of the product.

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: 10786682

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 Related Products by Product Action

View all VEGFR Inhibitors

Keywords: Vatalanib succinate, 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, Cytochrome, P450, 5680, Tocris Bioscience

2 Citations for Vatalanib succinate

Citations are publications that use Tocris products. Selected citations for Vatalanib succinate include:

Rasmussen et al (2018) Fish Scales Dictate the Pattern of Adult Skin Innervation and Vascularization. Dev Cell 46 344 PMID: 30032992

Jeffrey P et al (2022) Osteoblasts pattern endothelium and somatosensory axons during zebrafish caudal fin organogenesis. Development 149 PMID: 35129199


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Vatalanib succinate

VEGF Signaling Pathway

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.