Description
Vatalanib base can inhibit VEGFR-2 (KDR), VEGF-R1(FLT-1), Flk and c-Kit with IC50 of 37 nM, 77 nM, 270 nM and 730 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C20H15ClN4
Chemical Name
N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine dihydrochloride
Solubility
DMSO 85 mg/mL Water 10 mg/mL Ethanol 6 mg/mL
In vitro
Vatalanib base can inhibit VEGFR-2 (KDR), VEGF-R1(FLT-1), Flk and c-Kit with IC50 of 37 nM, 77 nM, 270 nM and 730 nM. Vatalanib base inhibits VEGF-induced autophosphorylation of kinase insert domain-containing receptor (KDR), endothelial cell proliferation, migration, and survival. Vatalanib base induces dose-dependent inhibition of VEGF and PDGF-induced angiogenesis in a growth factor implant model, as well as a tumor cell-driven angiogenesis.
In vivo
(1) Renal cell carcinoma (RCC):As a specific inhibitor of both VEGF-receptor tyrosine kinases, Vatalanib base potently inhibits tumor growth, metastases formation, and tumor vascularization in murine renal cell carcinoma. (2) MM cell lines: Vatalanib base acts both directly on MM cells and in the bone marrow microenvironment. Specifically, Vatalanib base (1-5 micro M) inhibits proliferation of MM cells by 50%. This effect of vatalanib base is dose dependent in both MM cell lines. Vatalanib base enhances the inhibitory effect of dexamethasone on growth of MM cells and can overcome the protective effect of interleukin 6 (IL-6) against dexamethasone-induced apoptosis. Vatalanib base (1 micro M) also blocks VEGF-induced migration of MM cells across an extracellular matrix. Importantly, Vatalanib base also inhibits the increased MM cell proliferation and increased IL-6 and VEGF secretion in cultures of MM cells adherent to bone marrow stem cells. (3) Malignant glioma cell lines:Early and delayed application of Vatalanib base in V(+) glioma-bearing animals resulted in a significant reduction of tumor size (71% and 36%, P (4) Models of rheumatoid arthritis:Vatalanib base treatment caused dose dependent reduction in the vascularity of the granulomatous air pouch model. Vatalanib base inhibited knee swelling by 40% in antigen-induced arthritis.
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