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Submit ReviewVatalanib 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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 46.49 | 100 |
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.
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 |
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
If you know of a relevant reference for Vatalanib succinate, please let us know.
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
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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