TYRPHOSTIN B7

Description

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors such as epidermal growth factor (EGF) or platelet-derived growth factor (PDGF) by blocking the phosphorylation of specific tyrosine residues. AG-370 is a selective inhibitor of PDGF receptor kinase with an IC₅₀ value of 20 μM in human bone marrow fibroblasts. It displays comparatively weak inhibition of the EGF receptor (IC₅₀ = 820 μM).

What are the applications of Application

AG-370 is a selective inhibitor of PDGFR kinase

Definition

ChEBI: AG-370 is a member of indoles.

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 [1].

References

[1] 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).