AG957-Tyrphostin-AG957-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE AG957 Cat. No.: HY-117718 CAS No.: 140674-76-6 Synonyms: Tyrphostin AG957; NSC 654705 分⼦式: C₁₅H₁₅NO₄ 分⼦量: 273.28 作⽤靶点: Bcr-Abl 作⽤通路: Protein Tyrosine Kinase/RTK 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 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 [1] [2]。 AG957抑制 p210bcr/abl 酶活性，IC50 为 2.9 μM [3]。 体外研究 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 p210BCR/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 sig