Vatalanib succinate  (Synonyms: PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate)

Vatalanib (PTK787) succinate is a potent and orally active VEGFR inhibitor with IC₅₀s of 37 nM, 77 nM, 270 nM, 660 nM, 730 nM, 1400 nM, and 580 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, respectively^[1].

Vatalanib (PTK787) inhibits VEGF-induced autophosphorylation of kinase insert domain-containing receptor (KDR), endothelial cell proliferation, migration, and survival in the nanomolar range in cell-based assays. In concentrations up to 1 µM, Vatalanib (PTK787) does not have any cytotoxic or antiproliferative effect on cells that do not express VEGF receptors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

After oral dosing (50 mg/kg) to mice, plasma concentrations of Vatalanib (PTK787) remain above 1 μM for more than 8 h. Vatalanib (PTK787) induces dose-dependent inhibition of VEGF and PDGF-induced angiogenesis in a growth factor implant model, as well as a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

464.90

C₂₄H₂₁ClN₄O₄

212142-18-2

ClC(C=C1)=CC=C1NC2=C3C(C=CC=C3)=C(CC4=CC=NC=C4)N=N2.OC(CCC(O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. J M Wood, 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 Apr 15;60(8):2178-89.  [Content Brief]