AG957

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity^[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC₅₀ of 2.9 μM for p210^bcr/abl autokinase activity^[3]. In Vitro: AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation^[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210^BCR/ABL kinase, on beta1 integrin function in CML progenitors^[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC^[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells^[2]. In Vivo: AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice^[4].