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AG957

CAS No. : 140674-76-6

MCE 站：AG957

产品活性：AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂，具有抗 BCR/ABL 酪氨酸激酶活性。AG957抑制 p210^bcr/abl 酶活性，IC₅₀ 为 2.9 μM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Bcr-Abl

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.Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210^BCR/ABL kinase, on beta1 integrin function in CML progenitors.
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC.
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.

In Vivo: AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice.

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