Overview
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Protect from light.
Alomone Labs Tyrphostin AG 1296 inhibits the kinase activity of PDGF receptor in 3T3-L1 cells.Cells were serum starved for 3 h. The cells were then incubated for 30 min with various concentrations of Tyrphostin AG 1296 (#T-770) and stimulated with 10 ng/ml PDGF-BB. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-PDGFR (upper panel) and with antiphospho ERK1/2 (lower panel). Inhibition of ERK1/2 phosphorylation was dose-dependent.
Tyrphostin AG1296 is a tyrosine kinase blocker which selectively inhibits platelet-derived growth factor (PDGF) a- and b-receptor kinases and the PDGF-dependent signaling in many cell types. Tyrphostin AG1296 also inhibits the PDGF dependent transactivation of the P2Y and Endothelin receptors-evoked cell proliferation and MAPK activation.1-4
This PDGF receptor (PDGFR) blocker has no effect on epidermal growth factor (EGF) receptor autophosphorylation; weak effects on DNA synthesis stimulated by insulin, by EGF, or by a combination of both; and over an order of magnitude weaker blocking effect on fibroblast growth factor-dependent (FGF) DNA synthesis.5-8 Tyrphostin AG1296 also potently inhibits the signaling of stem cell factor (SCF) receptor (c-Kit) and its upstream effector Kit receptor tyrosine kinase and the tyrosine kinase activity of FLT3-ITD which both have a strong sequence similarity with other members of the class III receptor tyrosine kinase but has no effect on the autophosphorylation of vascular endothelial growth factor (VEGF) receptor. 7,8
