IC50: 20 μM for PDGF receptor kinase in human bone marrow fibroblasts
AG-370 is a tyrphostin PDGFR inhibitor.
Protein tyrosine kinase inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of protein tyrosine kinases. Tyrphostins are a class of antiproliferative agents selectively inhibiting protein tyrosine kinases of key growth factors including epidermal growth factor or platelet-derived growth factor (PDGF) via blocking the phosphorylation of tyrosine residues.
In vitro: Previous study found that AG-370 inhibited PDGF receptor autophosphorylation and the tyrosine phosphorylation of intracellular protein substrates that coprecipitated with the PDGF receptor in digitonin-permeabilized fibroblasts and in intact fibroblasts. When compared with AG18, a potent EGF receptor blocker, AG370 was more efficient in inhibiting PDGF-induced proliferation of fibroblasts and phosphorylation of the intracellular protein substrates. Under the conditions in which AG370 could inhibit PDGF-induced mitogenesis and phosphorylation, AG18 did not alter [125I]PDGF internalization and enhance [125I]PDGF binding. These findings suggested that AG370 might have a therapeutic potential for treatment of diseases involving abnormal cellular proliferation induced by PDGF .
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
 Bryckaert, M. C.,Eldor, A.,Fontenay, M., et al. Inhibition of platelet-derived growth factor-induced mitogenesis and tyrosine kinase activity in cultured bone marrow fibroblasts by tyrphostins. Experimental Cell Research 199, 255-261 (1992).
|Physical Appearance||A crystalline solid|
|Storage||Store at -20°C|
|Solubility||≤30mg/ml in DMSO;30mg/ml in dimethyl formamide|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|